Domatinostat tosylate(Synonyms: 4SC-202)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Domatinostat tosylate (Synonyms: 4SC-202) 纯度: 99.66%

Domatinostat tosylate (4SC-202) 是一种 I 型 HDAC 抑制剂,能够抑制 HDAC1,HDAC2,和 HDAC3 的活性,IC50 值分别为 1.20 μM,1.12 μM 和 0.57 μM;同时能够抑制组蛋白赖氨酸特异性脱甲基酶1 (Lysine specific demethylase 1) 的活性。

Domatinostat tosylate(Synonyms: 4SC-202)

Domatinostat tosylate Chemical Structure

CAS No. : 1186222-89-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1636 In-stock
2 mg ¥800 In-stock
5 mg ¥1200 In-stock
10 mg ¥1800 In-stock
50 mg ¥5100 In-stock
100 mg ¥8150 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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  • Anti-Liver Cancer Compound Library

生物活性

Domatinostat tosylate (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1).

IC50 & Target[4]

HDAC-3

0.57 μM (IC50)

HDAC-2

1.12 μM (IC50)

HDAC-1

1.2 μM (IC50)

HDAC-11

9.7 μM (IC50)

HDAC-5

11.3 μM (IC50)

HDAC-10

21 μM (IC50)

HDAC-9

50 μM (IC50)

体外研究
(In Vitro)

Domatinostat tosylate significantly reduces proliferation of all epithelial and mesenchymal UC cell lines (IC50 0.15-0.51 μM), inhibits clonogenic growth and induces caspase activity[1]. Domatinostat tosylate provokes apoptosis activation in CRC cells, while caspase inhibitors (z-VAD-CHO and z-DVED-CHO) significantly alleviate Domatinostat tosylate-exerted cytotoxicity in CRC cells. Meanwhile, Domatinostat tosylate induces dramatic G2-M arrest in CRC cells. Further studies show that AKT activation might be an important resistance factor of Domatinostat tosylate. Domatinostat tosylate-induced cytotoxicity is dramatically potentiated with serum starvation, AKT inhibition (by perifosine or MK-2206), or AKT1-shRNA knockdown in CRC cells. On the other hand, exogenous expression of constitutively active AKT1 (CA-AKT1) decreases the sensitivity by Domatinostat tosylate in HT-29 cells. Notably, Domatinostat tosylate, at a low concentration, enhances oxaliplatin-induced in vitro anti-CRC activity[2]. Domatinostat tosylate treatment induces potent cytotoxic and proliferation-inhibitory activities against established HCC cell lines (HepG2, HepB3, SMMC-7721) and patient-derived primary HCC cells. Domatinostat tosylate induces apoptosis signal-regulating kinase 1 (ASK1) activation, causing it translocation to mitochondria and physical association with Cyp-D[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Oral gavage of Domatinostat tosylate inhibits HT-29 xenograft growth in nude mice, and when combined with oxaliplatin, its activity is further strengthened[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

619.71

Formula

C30H29N5O6S2

CAS 号

1186222-89-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : ≥ 51 mg/mL (82.30 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6137 mL 8.0683 mL 16.1366 mL
5 mM 0.3227 mL 1.6137 mL 3.2273 mL
10 mM 0.1614 mL 0.8068 mL 1.6137 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.03 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.03 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.03 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.03 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Pinkerneil M, et al. Evaluation of the Therapeutic Potential of the Novel Isotype Specific HDAC Inhibitor 4SC-202 in Urothelial Carcinoma Cell Lines. Target Oncol. 2016 Dec;11(6):783-798.

    [2]. S.W.Henning, et al. Preclinical characterization of 4SC-202, a noval isotype specific HDAC inhibitor.

    [3]. Zhijun H, et al. Pre-clinical characterization of 4SC-202, a novel class I HDAC inhibitor, against colorectal cancer cells. Tumour Biol. 2016 Aug;37(8):10257-67.

    [4]. Fu M, et al. 4SC-202 activates ASK1-dependent mitochondrial apoptosis pathway to inhibit hepatocellular carcinoma cells. Biochem Biophys Res Commun. 2016 Mar 4;471(2):267-73

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Ningetinib Tosylate(Synonyms: 对甲苯磺酸宁格替尼)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Ningetinib Tosylate (Synonyms: 对甲苯磺酸宁格替尼) 纯度: 99.92%

Ningetinib Tosylate 是一种有效的口服生物可用的小分子酪氨酸激酶抑制剂 (TKI),对 c-MetVEGFR-2AxlIC50 值分别为 6.7, 1.9 和 <1.0 nM。

Ningetinib Tosylate(Synonyms: 对甲苯磺酸宁格替尼)

Ningetinib Tosylate Chemical Structure

CAS No. : 1394820-77-9

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1363 In-stock
5 mg ¥850 In-stock
10 mg ¥1200 In-stock
50 mg ¥4200 In-stock
100 mg ¥7200 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

Ningetinib Tosylate is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.

IC50 & Target

VEGFR2

1.9 nM (IC50)

体外研究
(In Vitro)

Ningetinib Tosylate is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively. In cell-based functional assays, Ningetinib Tosylate (CT053PTSA) inhibits HGF and VEGF-stimulated HUVEC proliferation and microvascular angiogenesis in rat aortic rings with IC50 values of 8.6 and 6.3 nM, respectively[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

When single dosed orally (3 mg/kg) to U87MG tumor-bearing nude mice, Ningetinib Tosylate (CT053PTSA) potently inhibits the phosphorylation of c-Met and its downstream signaling kinases AKT and ERK1/2 for up to 6 hours in tumor tissues. In orthotopic U87MG human glioblastoma xenograft model, Ningetinib Tosylate prolongs the median survival time (MST) and yields significant increase in life-span value (ILS=32%, p=0.003) at an oral dose of 20 mg/kg/day (dosed 21 days) versus the vehicle-treated group[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

728.79

Formula

C38H37FN4O8S

CAS 号

1394820-77-9

中文名称

对甲苯磺酸宁格替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 33.33 mg/mL (45.73 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3721 mL 6.8607 mL 13.7214 mL
5 mM 0.2744 mL 1.3721 mL 2.7443 mL
10 mM 0.1372 mL 0.6861 mL 1.3721 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.43 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.43 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (3.43 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.43 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.43 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.43 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Ning Xi, et al. Abstract 1755: CT053PTSA, a novel c-MET and VEGFR2 inhibitor, potently suppresses angiogenesis and tumor growth. Cancer Res 2014;74(19 Suppl):Abstract nr 1755.

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Niraparib tosylate hydrate(Synonyms: MK-4827 tosylate hydrate)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Niraparib tosylate hydrate (Synonyms: MK-4827 tosylate hydrate)

Niraparib (MK-4827) tosylate hydrate 是高效的,具有生物口服利用度的 PARP1PARP2 抑制剂,IC50 分别为 3.8 nM 和 2.1 nM。Niraparib tosylate hydrate 抑制 DNA 损伤修复,诱导凋亡 (apoptosis) 并具有抗肿瘤活性。

Niraparib tosylate hydrate(Synonyms: MK-4827 tosylate hydrate)

Niraparib tosylate hydrate Chemical Structure

CAS No. : 1613220-15-7

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Niraparib tosylate hydrate 的其他形式现货产品:

Niraparib Niraparib tosylate

生物活性

Niraparib (MK-4827) tosylate hydrate is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib tosylate hydrate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity[1][2][3].

IC50 & Target

PARP-2

2.1 nM (IC50)

PARP-1

3.8 nM (IC50)

V-PARP

330 nM (IC50)

TANK-1

570 nM (IC50)

PARP-3

1300 nM (IC50)

体外研究
(In Vitro)

Niraparib (MK-4827) inhibits PARP activity with EC50=4 nM and EC90=45 nM in a whole cell assay. MK-4827 inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10-100 nM range. MK-4827 displays excellent PARP 1 and 2 inhibition with IC50=3.8 and 2.1 nM, respectively, and in a whole cell assay[1].
To validate that Niraparib (MK-4827) inhibits PARP in these cell lines, A549 and H1299 cells are treated with 1 μM MK-4827 for various times and measured PARP enzymatic activity using a chemiluminescent assay. The results show that Niraparib (MK-4827) inhibits PARP within 15 minutes of treatment reaching about 85% inhibition in the A549 cells at 1 h and about 55% inhibition at 1 h for the H1299 cells[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Niraparib (MK-4827) is well tolerated and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) is characterized by acceptable pharmacokinetics in rats with plasma clearance of 28 (mL/min)/kg, very high volume of distribution (Vdss=6.9 L/kg), long terminal half-life (t1/2=3.4 h), and excellent bioavailability, F=65%[1].
Niraparib (MK-4827) enhances radiation response of p53 mutant Calu-6 tumor in both cases, with the single daily dose of 50 mg/kg being more effective than 25 mg/kg given twice daily[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

510.61

Formula

C26H30N4O5S

CAS 号

1613220-15-7

中文名称

甲苯磺酸尼拉帕尼一水物

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Jones P, et al. Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J Med Chem. 2009 Nov 26;52(22):7170-85.

    [2]. Bridges KA, et al. Niraparib (MK-4827), a novel poly(ADP-Ribose) polymerase inhibitor, radiosensitizes human lung and breast cancer cells. Oncotarget. 2014 Jul 15;5(13):5076-86.

    [3]. Wang L, et al. MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation. Invest New Drugs. 2012 Dec;30(6):2113-20.

    [4]. Mirza MR, et al. Niraparib Maintenance Therapy in Platinum-Sensitive, Recurrent Ovarian Cancer. N Engl J Med. 2016 Dec 1;375(22):2154-2164.

Cell Assay

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Jones P, et al. Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J Med Chem. 2009 Nov 26;52(22):7170-85.

    [2]. Bridges KA, et al. Niraparib (MK-4827), a novel poly(ADP-Ribose) polymerase inhibitor, radiosensitizes human lung and breast cancer cells. Oncotarget. 2014 Jul 15;5(13):5076-86.

    [3]. Wang L, et al. MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation. Invest New Drugs. 2012 Dec;30(6):2113-20.

    [4]. Mirza MR, et al. Niraparib Maintenance Therapy in Platinum-Sensitive, Recurrent Ovarian Cancer. N Engl J Med. 2016 Dec 1;375(22):2154-2164.

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AZD3229 Tosylate

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

AZD3229 Tosylate  纯度: 98.54%

AZD3229 Tosylate 是一种有效的、广泛的突变型酪氨酸激酶受体 (KIT) 抑制剂,可用于开发研究胃肠道间质瘤。

AZD3229 Tosylate

AZD3229 Tosylate Chemical Structure

CAS No. : 2248003-71-4

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
5 mg ¥1850 In-stock
10 mg ¥2900 In-stock
25 mg ¥5300 In-stock
50 mg ¥8800 In-stock
100 mg ¥14800 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

AZD3229 Tosylate 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Targeted Diversity Library
  • Anti-Liver Cancer Compound Library

生物活性

AZD3229 Tosylate is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.

IC50 & Target

KIT[1].

体外研究
(In Vitro)

AZD3229 is a potent, pan-KIT mutant inhibitor with potent single digit nM growth inhibition against a diverse panel of mutant KIT driven Ba/F3 cell lines (GI50=1-50 nM). AZD3229 demonstrates potent single digit nM growth inhibition across a broad cell panel, with good margin to KDR-driven effects. Selectivity over KDR can be rationalised predominantly by the interaction of water molecules with the protein and ligand in the active site and its kinome selectivity is similar to the best of the approved GIST agents[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

651.71

Formula

C31H34FN7O6S

CAS 号

2248003-71-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (153.44 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5344 mL 7.6721 mL 15.3442 mL
5 mM 0.3069 mL 1.5344 mL 3.0688 mL
10 mM 0.1534 mL 0.7672 mL 1.5344 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Kettle JG, et al. Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. J Med Chem. 2018 Oct 11;61(19):8797-8810.

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Edoxaban tosylate(Synonyms: 依度沙班对甲苯磺酸盐; DU-176b)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Edoxaban tosylate (Synonyms: 依度沙班对甲苯磺酸盐; DU-176b) 纯度: 99.47%

Edoxaban tosylate (DU-176b) 是一种选择性,有效和口服活性的 factor Xa (FXa) 抑制剂,对游离 FXa 和凝血酶原的 Ki 分别为 0.561 nM 和 2.98 nM。Edoxaban tosylate 是一种抗凝剂,可用于预防中风。Edoxaban tosylate 还是一种凝血酶和凝血因子 IXaβ (FIXa) 的弱抑制剂,Ki 值分别为 6.00 μM 和 41.7 μM,对 FXa 的选择性超过 10000 倍。Edoxaban tosylate 具有抗血栓形成的特性,可用于血栓栓塞性疾病的研究。

Edoxaban tosylate(Synonyms: 依度沙班对甲苯磺酸盐; DU-176b)

Edoxaban tosylate Chemical Structure

CAS No. : 480449-71-6

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生物活性

Edoxaban tosylate (DU-176b) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban tosylate is an anticoagulant agent and can be used for stroke prevention. Edoxaban tosylate is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban tosylate has antithrombotic properties and has potential for thromboembolic diseases treatment[1][2][3].

IC50 & Target

Ki: 0.561 nM (Free FXa); 2.98 nM (Prothrombinase); 6.00 μM (Thrombin) and 41.7 μM (Factor IXaβ)[1]

体外研究
(In Vitro)

Edoxaban (DU-176b) also inhibits rat, cynomolgus monkey and rabbit FXa with Ki values of 6.90 nM, 0.715 nM and 0.457 nM, respectively[1].
Prothrombin time (PT), activated partial thromboplastin time (APTT) and thrombin time (TT) of human plasma are prolonged by Edoxaban (DU-176b) in a concentration-dependent manner, doubling PT and APTT at 0.256 and 0.508 μM, respectively. The double clotting time (CT2) for TT, however, was much higher (4.95 μM), reflecting its anti-thrombin activity. Thrombin-induced platelet aggregation is inhibited by a high concentration of Edoxaban (DU-176b) (IC50: 2.90 μM), reflecting its weak anti-thrombin activity[1].
Edoxaban is minimally metabolized (,4%) by the cytochrome P450 system (CYP3A4) and is a substrate for P-glycoprotein[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Edoxaban (DU-176b; 0.5-12.5 mg/kg; oral administration; Wistar rats) dose-dependently inhibits thrombus formation in rat thrombosis models[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wistar rats (210-240 g) with venous stasis thrombosis model[1]
Dosage: 0.5 mg/kg, 2.5 mg/kg, 12.5 mg/kg
Administration: Oral administration
Result: Dose-dependently inhibited thrombus formation in rat thrombosis models.

Clinical Trial

分子量

720.26

Formula

C31H38ClN7O7S2

CAS 号

480449-71-6

中文名称

依度沙班对甲苯磺酸盐;伊多塞班对甲苯磺酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL (138.84 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3884 mL 6.9419 mL 13.8839 mL
5 mM 0.2777 mL 1.3884 mL 2.7768 mL
10 mM 0.1388 mL 0.6942 mL 1.3884 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.47 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.47 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (3.47 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.47 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.47 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.47 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Furugohri T, et al. DU-176b, a potent and orally active factor Xa inhibitor: in vitro and in vivo pharmacological profiles. J Thromb Haemost. 2008 Sep;6(9):1542-9.

    [2]. Mendell J, Lee F, Chen S, The Effects of the Antiplatelet Agents, Aspirin and Naproxen, on Pharmacokinetics and Pharmacodynamics of the Anticoagulant Edoxaban, a Direct Factor Xa Inhibitor. J Cardiovasc Pharmacol. 2013 Apr 23. [Epub ahead of print]

    [3]. Stacy ZA, et al. Edoxaban: A Comprehensive Review of the Pharmacology and Clinical Data for the Management of Atrial Fibrillation and Venous Thromboembolism. Cardiol Ther. 2016 Jun;5(1):1-18.

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Sorafenib Tosylate(Synonyms: 甲苯磺酸索拉非尼; Bay 43-9006 Tosylate)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Sorafenib Tosylate (Synonyms: 甲苯磺酸索拉非尼; Bay 43-9006 Tosylate) 纯度: 99.75%

Sorafenib Tosylate (Bay 43-9006 Tosylate) 是一种有效的口服活性 Raf 抑制剂,对 Raf-1B-RafIC50 分别为 6 nM 和 20 nM。Sorafenib Tosylate 是一种多激酶抑制剂,对 VEGFR2VEGFR3PDGFRβFLT3c-KitIC50 分别为 90 nM,15 nM,20 nM,57 nM 和 58 nM。Sorafenib Tosylate 诱导细胞自噬 (autophagy) 和凋亡 (apoptosis),并具有抗肿瘤活性。Sorafenib Tosylate 也是一种 ferroptosis 激动剂。

Sorafenib Tosylate(Synonyms: 甲苯磺酸索拉非尼; Bay 43-9006 Tosylate)

Sorafenib Tosylate Chemical Structure

CAS No. : 475207-59-1

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥500 In-stock
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100 mg ¥850 In-stock
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生物活性

Sorafenib Tosylate (Bay 43-9006 Tosylate) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. SorafenibTosylate is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib Tosylate induces autophagy and apoptosis. Sorafenib Tosylate has anti-tumor activity. Sorafenib Tosylate is a ferroptosis activator[1].

IC50 & Target[1]

VEGFR3

20 nM (IC50)

Braf

22 nM (IC50)

Raf-1

6 nM (IC50)

VEGFR2

90 nM (IC50)

BrafV599E

38 nM (IC50)

PDGFRβ

57 nM (IC50)

c-Kit

68 nM (IC50)

Flt3

58 nM (IC50)

体外研究
(In Vitro)

Sorafenib Tosylate also inhibits BRAFwt (IC50=22 nM), BRAFV599E (IC50=38 nM), VEGFR-2 (IC50=90 nM), VEGFR-3 (IC50=20 nM), PDGFR-β (IC50=57 nM), c-KIT (IC50=68 nM), and Flt3 (IC50=58 nM) in biochemical assays[1]. Sorafenib-induced phosphorylation of c-Met, p70S6K and 4EBP1 is significantly reduced when 10-0505 cells are co-treated with anti-human anti-HGF antibody, suggesting that treatment with Sorafenib Tosylate leads to increased HGF secretion and activation of c-Met and mTOR targets[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Sorafenib Tosylate (10, 30, 50 and 100 mg/kg, orally) treatment inhibits the tumor growth of 06-0606 and 10-0505 xenografts in a dose-dependent manner (P<0.01). The growth rate of 06-0606 and 10-0505 xenografts is also significantly reduced by Sorafenib. The weights of 06-0606 tumors in mice that are treated with Sorafenib 50 mg/kg and 100 mg/kg are approximately 13% and 5% of the controls, respectively. 50 mg dose of Sorafenib significantly inhibits tumor growth in mice with lines 5-1318, 26-1004 and 10-0505 (P<0.01). For 50 mg dose, the T/C ratio, where T and C are the median weight (mg) of Sorafenib- and vehicle-treated tumors at the end of the treatment, respectively, for 06-0606, 26-1004, 5-1318, and 10-0505 xenografts is 0.13, 0.10, 0.12 and 0.49, respectively[2]. The survival rate is 73.3 % in Diethyl nitrosamine (DENA) group and 83.3 % in Sorafenib group compared to 100 % in the normal control group. DENA group shows a significant increase in liver index (1.51-fold increase, p<0.05) compared to normal control group, while treatment with Sorafenib shows significant decrease (p<0.05) in liver index when compared to DENA group. The liver index in Sorafenib group significantly decreases to lower than its value in the normal control[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

637.03

Formula

C28H24ClF3N4O6S

CAS 号

475207-59-1

中文名称

甲苯磺酸索拉非尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : ≥ 31 mg/mL (48.66 mM)

H2O : < 0.1 mg/mL (insoluble)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5698 mL 7.8489 mL 15.6978 mL
5 mM 0.3140 mL 1.5698 mL 3.1396 mL
10 mM 0.1570 mL 0.7849 mL 1.5698 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.08 mg/mL (3.27 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (3.27 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.27 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.27 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.27 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.27 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Wilhelm SM, et al. BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res. 2004 Oct 1;64(19):7099-109.

    [2]. Huynh H, et al. Sorafenib and rapamycin induce growth suppression in mouse models of hepatocellular carcinoma. J Cell Mol Med. 2009 Aug;13(8B):2673-83.

    [3]. El-Ashmawy NE, et al. Sorafenib effect on liver neoplastic changes in rats: more than a kinase inhibitor. Clin Exp Med. 2016 Apr 16.

    [4]. Zhu W, et al. Combination of sorafenib and Valproic acid synergistically induces cell apoptosis and inhibits hepatocellular carcinoma growth via down-regulating Notch3 and pAkt. Am J Cancer Res. 2017 Dec 1;7(12):2503-2514.

Kinase Assay
[1]

To test compound inhibition against various RAF kinase isoforms, Sorafenib is added to a mixture of Raf-1 (80 ng), wt BRAF, or V599E BRAF (80 ng) with MEK-1 (1 μg) in assay buffer [20 mM Tris (pH 8.2), 100 mM NaCl, 5 mM MgCl2, and 0.15% β-mercaptoethanol] at a final concentration of 1% DMSO. The RAF kinase assay (final volume of 50 μL) is initiated by adding 25 μL of 10 μM γ-[33P]ATP (400 Ci/mol) and incubated at 32°C for 25 minutes. Phosphorylated MEK-1 is harvested by filtration onto a phosphocellulose mat, and 1% phosphoric acid is used to wash away unbound radioactivity. After drying by microwave heating, a β-plate counter is used to quantify filter-bound radioactivity[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

The 10-0505, 06-0606, and 26-1004 tumors are finely minced and washed three times with modified Eagle medium (MEM). Cells are harvested by centrifuging at 800× g for 10 min. Cells are treated with 3 or 6 μM of Sorafenib in serum free MEM in the presence or absence of 5 μg/mL anti-human hepatocyte growth factor (HGF) antibody for 48 hrs. A total of 2 mL of conditioned medium from vehicle- or Sorafenib-treated (without anti-human antibody) is collected and concentrated using a VIVASPIN 20 and secreted HGF in conditioned medium is determined by western blotting[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2][3]

Mice[2]
For dose-response experiment, mice bearing the 06-0606 and 10-0505 xenografts are given four doses of Sorafenib (10, 30, 50 and 100 mg/kg daily) orally for 12 days. Each treatment group comprised of five mice. To investigate the antitumor effects of Sorafenib, mice bearing tumors are orally administered 50 mg/kg Sorafenib daily for 12 days. Each treatment group is comprised of 14 animals and each experiment is repeated at least twice. Treatment started on day 7 after tumor implantation. By this time, the HCC xenografts reached the size of approximately 100 mm3. To study the effects of Rapamycin plus Sorafenib on the growth of 10-0505 xenograft, mice bearing tumors (14 per group) are orally administered either 200 μL of vehicle, or 50 mg/kg of Sorafenib, or 1 mg/kg of Rapamycin, or Rapamycin plus Sorafenib daily for indicated days. Tumor growth is monitored at least twice weekly by Vernier caliper measurement of the length and width of tumor. Tumor volume is calculated as follows: [length×width2×π/6]. At the end of the study, the mice are killed with body and tumor weights being recorded, and the tumors harvested for analysis.
Rats[3]
In the study, 100- to 120-g male albino rats are utilized. After acclimatization period, rats are weighed and randomly divided into three groups: Group 1 (normal control group; n=10) is given the vehicle daily for 8 weeks. Group 2 (DENA group; n=15) receive i.p. single dose of 200 mg/kg DENA. Group 3 (Sorafenib group; n=12) is given Sorafenib orally at a dose of 10 mg/kg daily for 2 weeks, 6 weeks after DENA i.p. injection. At the end of the experiment (8 weeks), rats are weighed, anesthetized by ether, and killed, and their livers are dissected. Fresh liver is washed twice with ice-cold saline, dried on clean paper towel, and weighed. Liver index is calculated as liver weight (g)/final body weight (g)×100. The liver is divided into five portions: one portion is preserved in 10 % formalin for histopathological examination and the other portions are immediately frozen in liquid nitrogen and stored at −80°C.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Wilhelm SM, et al. BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res. 2004 Oct 1;64(19):7099-109.

    [2]. Huynh H, et al. Sorafenib and rapamycin induce growth suppression in mouse models of hepatocellular carcinoma. J Cell Mol Med. 2009 Aug;13(8B):2673-83.

    [3]. El-Ashmawy NE, et al. Sorafenib effect on liver neoplastic changes in rats: more than a kinase inhibitor. Clin Exp Med. 2016 Apr 16.

    [4]. Zhu W, et al. Combination of sorafenib and Valproic acid synergistically induces cell apoptosis and inhibits hepatocellular carcinoma growth via down-regulating Notch3 and pAkt. Am J Cancer Res. 2017 Dec 1;7(12):2503-2514.

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Valemetostat tosylate(Synonyms: DS-3201 tosylate)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Valemetostat tosylate (Synonyms: DS-3201 tosylate) 纯度: 99.91%

Valemetostat tosylate (DS-3201 tosylate) 是一种首创的 EZH1/2 抑制剂,用于复发/难治性周围 T 细胞淋巴瘤的研究。

Valemetostat tosylate(Synonyms: DS-3201 tosylate)

Valemetostat tosylate Chemical Structure

CAS No. : 1809336-93-3

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100 mg   询价  
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生物活性

Valemetostat tosylate (DS-3201 tosylate), a first-in-class EZH1/2 dual inhibitor, has the potential in the research of relapsed/refractory peripheral T-cell lymphoma[1].

IC50 & Target

EZH1/2[1]

Clinical Trial

分子量

660.22

Formula

C33H42ClN3O7S

CAS 号

1809336-93-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 125 mg/mL (189.33 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5146 mL 7.5732 mL 15.1465 mL
5 mM 0.3029 mL 1.5146 mL 3.0293 mL
10 mM 0.1515 mL 0.7573 mL 1.5146 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.15 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.15 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.15 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.15 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.15 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.15 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Daiichi Sankyo’s EZH1/2 Dual Inhibitor Valemetostat (DS-3201) Receives SAKIGAKE Designation for Treatment of Patients with Relapsed/Refractory Peripheral T-Cell Lymphoma from Japan MHLW.

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S-Adenosyl-L-methionine tosylate(Synonyms: S-Adenosyl methionine tosylate; Ademetionine tosylate; AdoMet tosylate)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

S-Adenosyl-L-methionine tosylate (Synonyms: S-Adenosyl methionine tosylate; Ademetionine tosylate; AdoMet tosylate) 纯度: ≥98.0%

S-Adenosyl-L-methionine tosylate (S-Adenosyl methionine tosylate) 是通过蛋氨酸腺苷转移酶的作用由蛋氨酸和 ATP 内源性生产的,是一种重要的具有口服活性的甲基供体。S-Adenosyl-L-methionine tosylate 是一种具有有效的抗抑郁作用的膳食补充剂,可用于缓解疼痛的研究,并可用于肝病和骨关节炎的研究。

S-Adenosyl-L-methionine tosylate(Synonyms: S-Adenosyl methionine tosylate; Ademetionine tosylate; AdoMet tosylate)

S-Adenosyl-L-methionine tosylate Chemical Structure

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10 mM * 1 mL in Water ¥825 In-stock
50 mg ¥750 In-stock
100 mg ¥1300 In-stock
500 mg ¥3900 In-stock
1 g   询价  
5 g   询价  

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生物活性

S-Adenosyl-L-methionine tosylate (S-Adenosyl methionine tosylate) is produced endogenously from methionine and ATP by action of the enzyme methionine adenosyltransferase and is an important orally active methyl group donor. S-Adenosyl-L-methionine tosylate is a dietary supplement with potent antidepressant and analgesic effects, and has the potential for liver disease and osteoarthritis research[1][2][3].

IC50 & Target

Human Endogenous Metabolite

 

体外研究
(In Vitro)

S-Adenosyl-L-methionine (Ademetionine) is involved in three main metabolic pathways: 1) methylation, as the principal source of methyl groups in the body; 2) transsulfuration, S-Adenosyl-L-methionine forms S-Adenosylhomocysteine (SAH) and then converted to homocysteine (Hcy) which can be converted to cystathionine then to cysteine and the sulfate (SO4) donated to other metabolic intermediates; and 3) aminopropylation, as S-Adenosyl-L-methionine plays an important role in the synthesis of polyamines which can eventually form and recycle methionine[2].
In vitro studies using human articular chondrocytes have shown S-Adenosyl-L-methionine-induced increases in proteoglycan synthesis and proliferation rates in rabbits[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Mice lacking methionine adenosyltransferase 1a (Mat1a) have reduced hepatic S-Adenosyl-L-methionine levels and develop oxidative stress, steatohepatitis, and hepatocellular carcinoma (HCC). However, injury and HCC also occur if hepatic S-Adenosyl-L-methionine level is excessive chronically. Thus a normal hepatic S-Adenosyl-L-methionine level is necessary to maintain liver health and prevent injury and HCC[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

570.64

Formula

C22H30N6O8S2

中文名称

腺苷蛋氨酸甲苯磺酸盐;丁二磺酸腺苷蛋氨酸甲苯磺酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
In Vitro: 

H2O : 250 mg/mL (438.10 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7524 mL 8.7621 mL 17.5242 mL
5 mM 0.3505 mL 1.7524 mL 3.5048 mL
10 mM 0.1752 mL 0.8762 mL 1.7524 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. G M Bressa. et al. S-adenosyl-l-methionine (SAMe) as antidepressant: meta-analysis of clinical studies. Acta Neurol Scand Suppl. 1994;154:7-14.

    [2]. Wadie I Najm, et al. S-adenosyl methionine (SAMe) versus celecoxib for the treatment of osteoarthritis symptoms: a double-blind cross-over trial. [ISRCTN36233495]. BMC Musculoskelet Disord. 2004 Feb 26;5:6.

    [3]. Shelly C Lu, et al. S-adenosylmethionine in liver health, injury, and cancer. Physiol Rev. 2012 Oct;92(4):1515-42.

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T-1101 tosylate(Synonyms: TAI-95 tosylate)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

T-1101 tosylate (Synonyms: TAI-95 tosylate) 纯度: 99.61%

T-1101 tosylate (TAI-95 tosylate) 是一种具有抗肿瘤活性的 Hec1/Nek2 抑制剂。T-1101 tosylate 对正常细胞、激酶和 hERG 无抑制效果。

T-1101 tosylate(Synonyms: TAI-95 tosylate)

T-1101 tosylate Chemical Structure

CAS No. : 2250404-95-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥6590 In-stock
5 mg ¥4500 In-stock
10 mg ¥7500 In-stock
50 mg 询价
100 mg 询价

* Please select Quantity before adding items.

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生物活性

T-1101 tosylate (TAI-95 tosylate) is a Hec1/Nek2 (Highly expressed in cancer 1 / NIMA-related kinase 2) inhibitor with antitumor activity. T-1101 tosylate is inactive toward normal cells, kinases and hERG[1]

IC50 & Target

Hec1/Nek2[1]

体外研究
(In Vitro)

T-1101 tosylate shows potent in vitro antiproliferative activity (IC50: 14.8-21.5 nM)[1].
T-1101 tosylate disrupts the Hec1/Nek2 protein–protein interaction in the cells[1].
T-1101 tosylate (1μM; 3-24 24 hours) decreases the level of Nek2 in a time-dependent manner[1].
T-1101 tosylate (1 µM; 24 hours) induces apoptosis[1].
T-1101 tosylate reduces amounts of cell-cycle related proteins cyclin A1, cyclin B1, and cyclin D1[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: HeLa cells
Concentration: 1 µM
Incubation Time: 24 hours
Result: Increased the amount of apoptotic marker proteins cleaved caspase-3 and PARP and decreased the amount of antiapoptotic proteins Mcl-1 and XIAP in HeLa cells.

Western Blot Analysis[1]

Cell Line: K562 cells
Concentration: 1 μM
Incubation Time: 3 hours, 6 hours, 16 hours, 24 hours
Result: Lowered the level of Nek2 in a time-dependent manner.

体内研究
(In Vivo)

T-1101 tosylate shows good oral bioavailability and thermal stability [1].
Oral co-administration of T-1101 tosylate (2.5 mg/kg; p.o.; twice per day) halves the dose of sorafenib (25 mg/kg to 12.5 mg/kg) required to exhibit comparable in vivo activity towards Huh-7 xenografts [1].
T-1101 tosylate (2.5 mg/kg; p.o.; twice per day) shows significant in vivo activity in mice bearing various human cancer xenografts[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SCID mice bearing human Huh-7, BT-474, MCF-7, and MDA-MB-231 xenografts[1]
Dosage: 25 mg/kg, 50 mg/kg
Administration: Oral administration; twice per day; 28 days
Result: Showed significant in vivo activity in mice bearing various human cancer xenografts.

Clinical Trial

分子量

665.80

Formula

C31H31N5O6S3

CAS 号

2250404-95-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 62.5 mg/mL (93.87 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5020 mL 7.5098 mL 15.0195 mL
5 mM 0.3004 mL 1.5020 mL 3.0039 mL
10 mM 0.1502 mL 0.7510 mL 1.5020 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.12 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.12 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.12 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.12 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Chuang SH, et al. Discovery of T-1101 tosylate as a first-in-class clinical candidate for Hec1/Nek2 inhibition in cancer therapy. Eur J Med Chem. 2020 Apr 1;191:112118.

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Niraparib tosylate(Synonyms: 尼拉帕尼对苯甲磺酸盐; MK-4827 tosylate)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Niraparib tosylate (Synonyms: 尼拉帕尼对苯甲磺酸盐; MK-4827 tosylate) 纯度: 99.81%

Niraparib tosylate (MK-4827 tosylate) 是一种高效的,具有生物口服利用度的 PARP1PARP2 抑制剂,IC50 分别为 3.8 和 2.1 nM。Niraparib tosylate 抑制 DNA 损伤修复,诱导凋亡 (apoptosis) 并具有抗肿瘤活性。

Niraparib tosylate(Synonyms: 尼拉帕尼对苯甲磺酸盐; MK-4827 tosylate)

Niraparib tosylate Chemical Structure

CAS No. : 1038915-73-9

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥672 In-stock
2 mg ¥550 In-stock
5 mg ¥620 In-stock
10 mg ¥1050 In-stock
50 mg ¥4100 In-stock
100 mg ¥5900 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity[1][2][3].

IC50 & Target

PARP-2

2.1 nM (IC50)

PARP-1

3.8 nM (IC50)

V-PARP

330 nM (IC50)

TANK-1

570 nM (IC50)

PARP-3

1300 nM (IC50)

体外研究
(In Vitro)

Niraparib (MK-4827) inhibits PARP activity with EC50=4 nM and EC90=45 nM in a whole cell assay. MK-4827 inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10−100 nM range. MK-4827 displays excellent PARP 1 and 2 inhibition with IC50=3.8 and 2.1 nM, respectively, and in a whole cell assay[1]. To validate that Niraparib (MK-4827) inhibits PARP in these cell lines, A549 and H1299 cells are treated with 1 μM Niraparib (MK-4827) for various times and measured PARP enzymatic activity using a chemiluminescent assay. The results show that Niraparib (MK-4827) inhibits PARP within 15 minutes of treatment reaching about 85% inhibition in the A549 cells at 1 h and about 55% inhibition at 1 h for the H1299 cells[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Niraparib (MK-4827) is well tolerated and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) is characterized by acceptable pharmacokinetics in rats with plasma clearance of 28 (mL/min)/kg, very high volume of distribution (Vdss=6.9 L/kg), long terminal half-life (t1/2=3.4 h), and excellent bioavailability, F=65%[1]. Niraparib (MK-4827) enhances radiation response of p53 mutant Calu-6 tumor in both cases, with the single daily dose of 50 mg/kg being more effective than 25 mg/kg given twice daily[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

492.59

Formula

C26H28N4O4S

CAS 号

1038915-73-9

中文名称

尼拉帕尼对苯甲磺酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 200 mg/mL (406.02 mM; Need ultrasonic)

H2O : 1 mg/mL (2.03 mM; heat to 50°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0301 mL 10.1504 mL 20.3009 mL
5 mM 0.4060 mL 2.0301 mL 4.0602 mL
10 mM 0.2030 mL 1.0150 mL 2.0301 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (5.08 mM); Clear solution

  • 2.

    请依序添加每种溶剂: 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.08 mM); Clear solution

  • 3.

    请依序添加每种溶剂: 1% DMSO    99% saline

    Solubility: ≥ 0.5 mg/mL (1.02 mM); Clear solution

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Jones P, et al. Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J Med Chem. 2009 Nov 26;52(22):7170-85.

    [2]. Bridges KA, et al. Niraparib (MK-4827), a novel poly(ADP-Ribose) polymerase inhibitor, radiosensitizes human lung and breast cancer cells. Oncotarget. 2014 Jul 15;5(13):5076-86.

    [3]. Wang L, et al. MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation. Invest New Drugs. 2012 Dec;30(6):2113-20.

    [4]. Mirza MR, et al. Niraparib Maintenance Therapy in Platinum-Sensitive, Recurrent Ovarian Cancer. N Engl J Med. 2016 Dec 1;375(22):2154-2164.

Cell Assay
[2]

The inhibition of PARP is analyzed in A549 and H1299 cells using the HT Universal Chemiluminescent PARP Assay Kit. Briefly, cells are treated with DMSO or 1 μM Niraparib (MK-4827) for 15, 30, 60, or 120 minutes, trypsinized, and transferred to a pre-chilled tube. The cells are washed twice with ice cold PBS and resuspended in cold PARP extraction buffer. The cell suspensions are incubated on ice for 30 minutes with periodic vortexing to disrupt the cell membrane. The suspensions are centrifuged and the supernatant transferred to a pre-chilled tube on ice. The histone coated wells of the 96-well plate are rehydrated with 1X PARP buffer and incubated at room temperature for 30 minutes. The PARP buffer is removed and 20 μg of protein as determined by the Bio-Rad Protein Assay is added to each well followed by diluted PARP-HSA enzyme and 1X PARP buffer. The strip wells are then incubated at room temperature for 60 minutes, washed twice with PBS containing 0.1% Triton X-100, and then washed with PBS. Diluted Strep-HRP is added to the strip wells and incubated for 60 minutes at room temperature. The wells are washed again as before. Equal volumes of PeroxyGlow A and B are combined and added to the wells and chemiluminescent readings are obtained immediately using a plate-reader[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Mice[3]
Female nude mice (Ncr Nu/Nu) are randomly assigned to treatment groups consisting of 5 to 8 mice each when tumors grew to 6.0 mm in diameter at which time treatment with MK-4827 is initiated. MK-4827 is given at a dose of 25 mg/kg twice daily or 50 mg/kg once daily for either 21 days or is discontinued at 9 days from the time tumors reached 8 mm in diameter. Fractionated local tumor irradiation (XRT) is given when tumors reach 8.0 mm in diameter (7.7-8.2 mm). Radiation (2 Gy per fraction) is delivered to the tumor-bearing leg of mice once daily for 14 consecutive days or twice daily for 7 consecutive days using a small-animal irradiator consisting of two parallel-opposed 137Cs sources, at a dose rate of 5 Gy/min. During irradiation un-anesthetized mice are mechanically immobilized in a jig so that the tumor is centered within a 3.0 cm diameter radiation field and the animal’s body shielded from radiation exposure. On the day when both MK-4827 and radiation are given, drug is administered 1 h before the first radiation dose of the day.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Jones P, et al. Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J Med Chem. 2009 Nov 26;52(22):7170-85.

    [2]. Bridges KA, et al. Niraparib (MK-4827), a novel poly(ADP-Ribose) polymerase inhibitor, radiosensitizes human lung and breast cancer cells. Oncotarget. 2014 Jul 15;5(13):5076-86.

    [3]. Wang L, et al. MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation. Invest New Drugs. 2012 Dec;30(6):2113-20.

    [4]. Mirza MR, et al. Niraparib Maintenance Therapy in Platinum-Sensitive, Recurrent Ovarian Cancer. N Engl J Med. 2016 Dec 1;375(22):2154-2164.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

LY-2584702 tosylate salt

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

LY-2584702 tosylate salt  纯度: 98.12%

LY-2584702 tosylate salt 是一种 ATP 竞争性的选择性 p70S6K 抑制剂,IC50 为 4 nM。LY-2584702 抑制 S6K1IC50 为 2 nM。

LY-2584702 tosylate salt

LY-2584702 tosylate salt Chemical Structure

CAS No. : 1082949-68-5

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1114 In-stock
5 mg ¥820 In-stock
10 mg ¥1200 In-stock
50 mg ¥3600 In-stock
100 mg ¥5600 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

LY-2584702 tosylate salt 相关产品

相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
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  • Kinase Inhibitor Library
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  • Clinical Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Targeted Diversity Library

生物活性

LY-2584702 tosylate salt is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM. In S6K1 enzyme assay, the IC50 of LY-2584702 is 2 nM.

IC50 & Target

S6K1

2 nM (IC50)

p70S6K

4 nM (IC50)

体外研究
(In Vitro)

LY-2584702 (LY2584702) inhibits phosphorylation of the S6 ribosomal protein (pS6) in HCT116 colon cancer cells with an IC50 of 0.1-0.24 μM[1]. In S6K1 enzyme assay, the IC50 of LY-2584702 (LY2584702) is 2 nM. For pS6 inhibition in cells, the IC50=100 nM. LY-2584702 has some activity against the S6K-related kinases MSK2 and RSK at high concentrations (enzyme assay IC50=58-176 nM). LY-2584702 inhibits S6K activity in EOMA cells, as determined by the phosphorylation of its downstream effector S6, in a dose-dependent manner[2]. Proliferation of A549 is significantly inhibited by LY-2584702 (LY2584702) treating over 24 h at 0.1 μM (P<0.05); and the trend of decline is more conspicuous with longer treatment and/or with the increased drug concentration (all P<0.05). Similar results are also observed in SK-MES-1, although the obvious inhibition is led by LY-2584702 at 0.6 μM (P<0.05), much higher than that of A549[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

LY-2584702 demonstrates significant single-agent efficacy in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models at two dose levels of 2.5 mg/kg twice daily (BID) and 12.5 mg/kg BID. LY-2584702 demonstrates statistically significant tumour growth reduction at TMED50 (threshold minimum effective dose 50%) (2.3 mg/kg) and TMED90 (10 mg/kg) in the HCT116 colon carcinoma xenograft model[1]. To examine the role of S6K in vivo, EOMA cells expressing shAkt3 are implanted in nu/nu mice, then treated for 14 days with LY-2584702 or Rapamycin. Analysis of tumors removed after 14 days shows that LY-2584702 inhibits S6 phosphorylation almost as effectively as Rapamycin. Loss of Akt3 increases tumor growth as compared with pLKO. LY-2584702 treatment alone does not significantly affect the growth of pLKO tumors. However, LY-2584702 significantly reduces the growth of tumors with shAkt3[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

617.62

Formula

C28H27F4N7O3S

CAS 号

1082949-68-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 10.25 mg/mL (16.60 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6191 mL 8.0956 mL 16.1912 mL
5 mM 0.3238 mL 1.6191 mL 3.2382 mL
10 mM 0.1619 mL 0.8096 mL 1.6191 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1 mg/mL (1.62 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (1.62 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 1 mg/mL (1.62 mM); Suspended solution; Need ultrasonic

    此方案可获得 1 mg/mL (1.62 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 1 mg/mL (1.62 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (1.62 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Tolcher A, et al. A phase I trial of LY2584702 tosylate, a p70 S6 kinase inhibitor, in patients with advanced solid tumors. Eur J Cancer. 2014 Mar;50(5):867-75.

    [2]. Phung TL, et al. Akt1 and akt3 exert opposing roles in the regulation of vascular tumor growth. Cancer Res. 2015 Jan 1;75(1):40-50.

    [3]. Chen B, et al. Hyperphosphorylation of RPS6KB1, rather than overexpression, predicts worse prognosis in non-small cell lung cancer patients. PLoS One. 2017 Aug 9;12(8):e0182891.

Cell Assay
[3]

LY-2584702 is fully dissolved in 20 mL 10% DMSO and reserved at -80°C. When conducted the experiments in vitro, LY-2584702 is further diluted in 0.5% Tween 80, 5% propylene glycol and 30% PEG400 to reach different DMSO concentrations of 0.1 μM, 0.2 μM, 0.6 μM, and 1.0 μM. Cell Counting Kit-8 (CCK-8) is used to measure the cells proliferation in vitro. Cell lines A549 and SK-MES-1 treated by LY-2584702 for 24 h with different concentrations are seeded in 96-well plates at a density of 5×103 per well, with six repeats. DMSO treated, or in other words, the concentration of LY-2584702 of 0 is used as negative control. Cells absorbance at 450 nm is detected every 24 h after seeding to measure the proliferative activities[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice[2]
LY-2584702 is prepared in 0.25% Tween-80 and 0.05% antifoam, and administered orally to mice (12.5 mg/kg twice daily). EOMA cells (0.3×106) are injected subcutaneously in 6- to 8-week-old nu/nu female mice (2 sites/mouse, 4-5 mice/group). Tumor size is measured daily. For drug treatment, when tumors reach 0.01 cm3 in size, the animals are treated with vehicle control or LY-2584702 (12.5 mg/kg twice daily, oral dosing). Tumor size is measured every 3 to 4 days[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Tolcher A, et al. A phase I trial of LY2584702 tosylate, a p70 S6 kinase inhibitor, in patients with advanced solid tumors. Eur J Cancer. 2014 Mar;50(5):867-75.

    [2]. Phung TL, et al. Akt1 and akt3 exert opposing roles in the regulation of vascular tumor growth. Cancer Res. 2015 Jan 1;75(1):40-50.

    [3]. Chen B, et al. Hyperphosphorylation of RPS6KB1, rather than overexpression, predicts worse prognosis in non-small cell lung cancer patients. PLoS One. 2017 Aug 9;12(8):e0182891.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

甲苯磺酰基 PEG, mPEG-Tosylate, ,Tosyl PEG, mPEG-Tosylate,

甲苯磺酰基 PEG, mPEG-Tosylate

MW 1000 Da

有货

甲苯磺酰基 PEG, mPEG-Tosylate, &#x20;,Tosyl PEG, mPEG-Tosylate,

品牌:Jinpan
Tosyl PEG, mPEG-Tosylate

MSDS

质检证书(CoA)

相似产品

货号 (SKU) 包装规格 是否现货 价格 数量
T164401-100mg 100mg 期货 甲苯磺酰基 PEG, mPEG-Tosylate, &#x20;,Tosyl PEG, mPEG-Tosylate,  
T164401-500mg 500mg 期货 甲苯磺酰基 PEG, mPEG-Tosylate, &#x20;,Tosyl PEG, mPEG-Tosylate,  
T164401-2.5g 2.5g 期货 甲苯磺酰基 PEG, mPEG-Tosylate, &#x20;,Tosyl PEG, mPEG-Tosylate,  

基本信息

产品名称 甲苯磺酰基 PEG, mPEG-Tosylate
英文名称 Tosyl PEG, mPEG-Tosylate
规格或纯度 MW 1000 Da
运输条件 常规运输

一般描述

Tosyl functionctional PEG is an amino (-NH2) group reactive PEG derivative that can be used to modify protein, peptide or any other surfaces with available amino groups. Tosyl PEGs react readily with amine groups at a pH of from 8.0 to 9.5.

Tosyl functionctional PEG is an amino (-NH2) group reactive PEG derivative that can be used to modify protein, peptide or any other surfaces with available amino groups. Tosyl PEGs react readily with amine groups at a pH of from 8.0 to 9.5.

相关属性

溶解性 Off-white/white solid or viscous liquid depends on molecule weight;Soluble in regular aqeous solution as well as most organic solvents;
品牌 Jinpan

甲苯磺酰基 PEG, mPEG-Tosylate, ,Tosyl PEG, mPEG-Tosylate,

甲苯磺酰基 PEG, mPEG-Tosylate

MW 5000 Da

有货

甲苯磺酰基 PEG, mPEG-Tosylate, &#x20;,Tosyl PEG, mPEG-Tosylate,

品牌:Jinpan
Tosyl PEG, mPEG-Tosylate

MSDS

质检证书(CoA)

相似产品

货号 (SKU) 包装规格 是否现货 价格 数量
T164405-1g 1g 期货 甲苯磺酰基 PEG, mPEG-Tosylate, &#x20;,Tosyl PEG, mPEG-Tosylate,  
T164405-5g 5g 期货 甲苯磺酰基 PEG, mPEG-Tosylate, &#x20;,Tosyl PEG, mPEG-Tosylate,  

基本信息

产品名称 甲苯磺酰基 PEG, mPEG-Tosylate
英文名称 Tosyl PEG, mPEG-Tosylate
规格或纯度 MW 5000 Da
运输条件 常规运输

一般描述

Tosyl functionctional PEG is an amino (-NH2) group reactive PEG derivative that can be used to modify protein, peptide or any other surfaces with available amino groups. Tosyl PEGs react readily with amine groups at a pH of from 8.0 to 9.5.

Tosyl functionctional PEG is an amino (-NH2) group reactive PEG derivative that can be used to modify protein, peptide or any other surfaces with available amino groups. Tosyl PEGs react readily with amine groups at a pH of from 8.0 to 9.5.

相关属性

溶解性 Off-white/white solid or viscous liquid depends on molecule weight;Soluble in regular aqeous solution as well as most organic solvents;
品牌 Jinpan

甲苯磺酰基 PEG, mPEG-Tosylate, ,Tosyl PEG, mPEG-Tosylate,

甲苯磺酰基 PEG, mPEG-Tosylate

MW 10000 Da

有货

甲苯磺酰基 PEG, mPEG-Tosylate, &#x20;,Tosyl PEG, mPEG-Tosylate,

品牌:Jinpan
Tosyl PEG, mPEG-Tosylate

MSDS

质检证书(CoA)

相似产品

货号 (SKU) 包装规格 是否现货 价格 数量
T164402-1g 1g 期货 甲苯磺酰基 PEG, mPEG-Tosylate, &#x20;,Tosyl PEG, mPEG-Tosylate,  

基本信息

产品名称 甲苯磺酰基 PEG, mPEG-Tosylate
英文名称 Tosyl PEG, mPEG-Tosylate
规格或纯度 MW 10000 Da
运输条件 常规运输

一般描述

Tosyl functionctional PEG is an amino (-NH2) group reactive PEG derivative that can be used to modify protein, peptide or any other surfaces with available amino groups. Tosyl PEGs react readily with amine groups at a pH of from 8.0 to 9.5.

Tosyl functionctional PEG is an amino (-NH2) group reactive PEG derivative that can be used to modify protein, peptide or any other surfaces with available amino groups. Tosyl PEGs react readily with amine groups at a pH of from 8.0 to 9.5.

相关属性

溶解性 Off-white/white solid or viscous liquid depends on molecule weight;Soluble in regular aqeous solution as well as most organic solvents;
品牌 Jinpan

甲苯磺酰基 PEG, mPEG-Tosylate, ,Tosyl PEG, mPEG-Tosylate,

甲苯磺酰基 PEG, mPEG-Tosylate

MW 2000 Da

有货

甲苯磺酰基 PEG, mPEG-Tosylate, &#x20;,Tosyl PEG, mPEG-Tosylate,

品牌:Jinpan
Tosyl PEG, mPEG-Tosylate

MSDS

质检证书(CoA)

相似产品

货号 (SKU) 包装规格 是否现货 价格 数量
T164403-1g 1g 期货 甲苯磺酰基 PEG, mPEG-Tosylate, &#x20;,Tosyl PEG, mPEG-Tosylate,  

基本信息

产品名称 甲苯磺酰基 PEG, mPEG-Tosylate
英文名称 Tosyl PEG, mPEG-Tosylate
规格或纯度 MW 2000 Da
运输条件 常规运输

一般描述

Tosyl functionctional PEG is an amino (-NH2) group reactive PEG derivative that can be used to modify protein, peptide or any other surfaces with available amino groups. Tosyl PEGs react readily with amine groups at a pH of from 8.0 to 9.5.

Tosyl functionctional PEG is an amino (-NH2) group reactive PEG derivative that can be used to modify protein, peptide or any other surfaces with available amino groups. Tosyl PEGs react readily with amine groups at a pH of from 8.0 to 9.5.

相关属性

溶解性 Off-white/white solid or viscous liquid depends on molecule weight;Soluble in regular aqeous solution as well as most organic solvents;
品牌 Jinpan

甲苯磺酰基 PEG, mPEG-Tosylate, ,Tosyl PEG, mPEG-Tosylate,

甲苯磺酰基 PEG, mPEG-Tosylate

MW 20000 Da

有货

甲苯磺酰基 PEG, mPEG-Tosylate, &#x20;,Tosyl PEG, mPEG-Tosylate,

品牌:Jinpan
Tosyl PEG, mPEG-Tosylate

MSDS

质检证书(CoA)

相似产品

货号 (SKU) 包装规格 是否现货 价格 数量
T164404-1g 1g 期货 甲苯磺酰基 PEG, mPEG-Tosylate, &#x20;,Tosyl PEG, mPEG-Tosylate,  

基本信息

产品名称 甲苯磺酰基 PEG, mPEG-Tosylate
英文名称 Tosyl PEG, mPEG-Tosylate
规格或纯度 MW 20000 Da
运输条件 常规运输

一般描述

Tosyl functionctional PEG is an amino (-NH2) group reactive PEG derivative that can be used to modify protein, peptide or any other surfaces with available amino groups. Tosyl PEGs react readily with amine groups at a pH of from 8.0 to 9.5.

Tosyl functionctional PEG is an amino (-NH2) group reactive PEG derivative that can be used to modify protein, peptide or any other surfaces with available amino groups. Tosyl PEGs react readily with amine groups at a pH of from 8.0 to 9.5.

相关属性

溶解性 Off-white/white solid or viscous liquid depends on molecule weight;Soluble in regular aqeous solution as well as most organic solvents;
品牌 Jinpan

TMPyP4 tosylate(Synonyms: TMP 1363)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

TMPyP4 tosylate (Synonyms: TMP 1363) 纯度: ≥98.0%

TMPyP4 tosylate (TMP 1363) 是一种四链体 (G-quadruplex) 特异性配体,可抑制 G-四链体和 IGF-1 之间的相互作用。TMPyP4 tosylate (TMP 1363) 是一种端粒酶 (telomerase) 抑制剂,在骨肉瘤细胞系中具有抗肿瘤作用。

TMPyP4 tosylate(Synonyms: TMP 1363)

TMPyP4 tosylate Chemical Structure

CAS No. : 36951-72-1

规格 价格 是否有货 数量
100 mg ¥1200 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand, which inhibits the interaction between G-quadruplexes and IGF-1[1]. TMPyP4 tosylate (TMP 1363) is a telomerase inhibitor with antitumor effects in osteosarcoma cell lines[2].

IC50 & Target

G-quadruplex[2]
Telomerase[2]

分子量

1363.60

Formula

C72H66N8O12S4

CAS 号

36951-72-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : 25 mg/mL (18.33 mM; Need ultrasonic)

DMSO : 10 mg/mL (7.33 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.7334 mL 3.6668 mL 7.3335 mL
5 mM 0.1467 mL 0.7334 mL 1.4667 mL
10 mM 0.0733 mL 0.3667 mL 0.7334 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1 mg/mL (0.73 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (0.73 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1 mg/mL (0.73 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (0.73 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Chen H, et al. Insuline-like growth factor type I selectively binds to G-quadruplex structures. Biochim Biophys Acta Gen Subj. 2019 Jan;1863(1):31-38.

    [2]. Fujimori J, et al. Antitumor effects of telomerase inhibitor TMPyP4 in osteosarcoma cell lines. J Orthop Res. 2011 Nov;29(11):1707-11.

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Milademetan tosylate hydrate(Synonyms: DS-3032b; DS-3032 tosylate hydrate)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Milademetan tosylate hydrate (Synonyms: DS-3032b; DS-3032 tosylate hydrate) 纯度: 98.21%

Milademetan (DS-3032) tosylate hydrate 是特异性的、具有口服活性的 MDM2 抑制剂,用于急性髓系白血病和实体肿瘤的研究。Milademetan (DS-3032) tosylate hydrate 可诱导 G1 细胞周期阻滞、衰老和凋亡。

Milademetan tosylate hydrate(Synonyms: DS-3032b; DS-3032 tosylate hydrate)

Milademetan tosylate hydrate Chemical Structure

CAS No. : 2095625-97-9

规格 价格 是否有货 数量
5 mg ¥5800 In-stock
10 mg ¥9800 In-stock
25 mg ¥20000 In-stock
50 mg ¥33500 In-stock
100 mg ¥56000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

Milademetan (DS-3032) tosylate hydrate is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) tosylate hydrate induces G1 cell cycle arrest, senescence and apoptosis[1][2].

体外研究
(In Vitro)

Milademetan (DS-3032) can stabilize TP53 and selectively induce CDKNA1, BAX and MDM2 expression in neuroblastoma cells with wild-type TP53[3].
Milademetan (DS-3032b) treatment enhances TP53 target gene expression and induces G1 cell cycle arrest, senescence and apoptosis[3].
Milademetan (DS-3032b, 0-2000 nM) treatment selectively inhibits viability, proliferation and migration of neuroblastoma cells with wildtype TP53 independently of MYCN status[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[4]

Cell Line: SK-N-SH, SH-SY5Y, IMR32, IMR5 and LAN5 cell lines.
Concentration: 0-2000 nM.
Incubation Time: 24-72 h.
Result: Reduced viability in a dose- and time-dependent manner.
Exhibited IC50 values of 21.9 nM, 17.7 nM, 52.63 nM, 25.7 nM and 44.1 nM in SK-N-SH, SH-SY5Y, IMR32, IMR5 and LAN5 cell lines, respectively (72 h).

体内研究
(In Vivo)

Milademetan (DS-3032b, 50 mg/kg, oral gavage) delays tumor growth and improves survival in mice xenografted with neuroblastoma cells with functional TP53[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SH-SY5Y xenograft tumors in nude mice[4].
Dosage: 50 mg/kg.
Administration: Oral gavage for 30 consecutive days with an alternating schedule of 4 days of daily treatment with oral gavages followed by 2 days without treatment (4+2).
Result: Survival in the mouse cohort was significantly prolonged.
Reduced neuroblastoma xenograft tumor growth by activating TP53 signaling.

Clinical Trial

分子量

808.74

Formula

C37H44Cl2FN5O8S

CAS 号

2095625-97-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

DMSO : 50 mg/mL (61.82 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.2365 mL 6.1825 mL 12.3649 mL
5 mM 0.2473 mL 1.2365 mL 2.4730 mL
10 mM 0.1236 mL 0.6182 mL 1.2365 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 5 mg/mL (6.18 mM); Suspended solution; Need ultrasonic

    此方案可获得 5 mg/mL (6.18 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 5 mg/mL (6.18 mM); Suspended solution; Need ultrasonic

    此方案可获得 5 mg/mL (6.18 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 5 mg/mL (6.18 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (6.18 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. ARYL SULFONOHYDRAZIDES. WO 2017069289 A1.

    [2]. M.M. Gounder, et al. Milademetan, an oral MDM2 inhibitor, in well-differentiated/dedifferentiated liposarcoma: results from a phase 1 study in patients with solid tumors or lymphomas. European Journal of Cancer 138S2 (2020) S1–S62.

    [3]. Li, Yangbing, et al. Development of novel PROTAC Small-Molecule Degraders of MDM2 Protein and Peptidomimetic Inhibitors Targeting WDR5-MLL1 Protein-Protein Interaction.

    [4]. Viktor Arnhold, et al. Reactivating TP53 signaling by the novel MDM2 inhibitor DS-3032b as a therapeutic option for high-risk neuroblastoma. ncotarget. 2018 Jan 5; 9(2): 2304–2319.

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Dactolisib Tosylate(Synonyms: BEZ235 Tosylate; NVP-BEZ 235 Tosylate)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Dactolisib Tosylate (Synonyms: BEZ235 Tosylate; NVP-BEZ 235 Tosylate) 纯度: 99.88%

Dactolisib Tosylate (BEZ235 Tosylate) 是PI3KmTOR的双重激酶抑制剂,对PI3Kα, β, γ, δ 的IC50值分别为4, 75, 7, 5 nM。Dactolisib Tosylate (BEZ235 Tosylate) 抑制 mTORC1mTORC2

Dactolisib Tosylate(Synonyms: BEZ235 Tosylate; NVP-BEZ 235 Tosylate)

Dactolisib Tosylate Chemical Structure

CAS No. : 1028385-32-1

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥500 In-stock
10 mg ¥450 In-stock
50 mg ¥950 In-stock
100 mg ¥1450 In-stock
200 mg ¥2100 In-stock
500 mg ¥3900 In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

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生物活性

Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.

IC50 & Target

p110α

4 nM (IC50)

p110β

75 nM (IC50)

p110δ

7 nM (IC50)

p110γ

5 nM (IC50)

p110α-H1047R

4.6 nM (IC50)

p110α-E545K

5.7 nM (IC50)

mTOR

20.7 nM (IC50)

mTORC1

 

mTORC2

 

Autophagy

 

体外研究
(In Vitro)

Dactolisib (BEZ235) is an imidazo[4,5-c]quinoline derivative that inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes. The IC50s for PI3Kα, β, γ, δ are 4, 75, 7, 5 nM, respectively. It is also found to be as active against the mutant PI3KαE545K or PI3KαH1047R with IC50s of 5.7 and 4.6 nM, respectively. In human tumor cell lines, it is able to effectively and specifically block the dysfunctional activation of the PI3K pathway, inducing G1 arrest. PTEN-null cell lines PC3M and U87MG shows a dose-dependent reduction in cell proliferation when treated with increasing concentrations of Dactolisib (BEZ235), with an average GI50 of 10 to 12 nM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Dactolisib (BEZ235) is well tolerated, displays disease stasis when administered orally, and enhances the efficacy of other anticancer agents. At a dose of 50 mg/kg, Dactolisib (BEZ235) appears rapidly in plasma with a Cmax of 1.68 μM at 0.5 h and a C24h of 0.03 μM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

641.74

Formula

C37H31N5O4S

CAS 号

1028385-32-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 34 mg/mL (52.98 mM; Need ultrasonic and warming)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5583 mL 7.7913 mL 15.5826 mL
5 mM 0.3117 mL 1.5583 mL 3.1165 mL
10 mM 0.1558 mL 0.7791 mL 1.5583 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 50% PEG300    50% saline

    Solubility: 16.67 mg/mL (25.98 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 1 mg/mL (1.56 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (1.56 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Maira SM, et al. Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. Mol Cancer Ther, 2008, 7(7), 1851-1863.

Animal Administration
[1]

Mice: The NVP-Dactolisib (BEZ235) powder is dissolved in NMP on sonication, and the remaining volume of polyethylene glycol 300 is added to a concentration of 5 mg/mL. The application volume is 10 mL/kg. For analytics, frozen tissues are minced and then homogenized in an equal volume of ice-cold PBS and centrifugation, supernatants are analyzed. Samples are then eluted with a linear gradient of 10% to 90% (v/v) acetonitrile in water containing 0.05% (v/v) trifluoroacetic acid over a period of 20 min at a flow rate of 1 mL/min. The compounds are detected by UV absorbance at 340 nm, and concentrations are determined by the external standard method using peak heights[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Maira SM, et al. Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. Mol Cancer Ther, 2008, 7(7), 1851-1863.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务