生物活性分子抑制剂Sulfatinib(Synonyms: HMPL-012)

生物活性分子抑制剂 特异性抑制剂 激动剂 化合物库 重组蛋白 Sulfatinib (Synonyms: HMPL-012) 纯度: 98.01%

Sulfatinib (HMPL-012) 是一种有效且高度选择性的针对 VEGFR1/2/3FGFR1CSF1R 的酪氨酸激酶抑制剂,IC50 值在1 到 24 nM之间。

Sulfatinib(Synonyms: HMPL-012)

Sulfatinib Chemical Structure

CAS No. : 1308672-74-3

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10 mM * 1 mL in DMSO ¥2009 In-stock
1 mg ¥900 In-stock
5 mg ¥1900 In-stock
10 mg ¥2900 In-stock
50 mg ¥8900 In-stock
100 mg ¥14000 In-stock
200 mg   询价  
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生物活性

Sulfatinib (HMPL-012) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC50s of in a range of 1 to 24 nM.

IC50 & Target[1]

VEGFR1

 

VEGFR2

 

VEGFR3

 

FGFR1

 

CSF1R

 

体外研究
(In Vitro)

Sulfatinib inhibits VEGFR1, 2, and 3, FGFR1 and CSF1R kinases with IC50s in a range of 1 to 24 nM, and it strongly blocks VEGF induced VEGFR2 phosphorylation in HEK293KDR cells and CSF1 stimulated CSF1R phosphorylation in RAW264.7 cells with IC50 of 2 and 79 nM, respectively. Sulfatinib also attenuates VEGF or FGF stimulated HUVEC cells proliferation with IC50< 50 nM[1]. Also, it is a hERG inhibitor with IC50 of 6.8 μM in CHO cell[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)

In animal studies, a single oral dosing of Sulfatinib inhibits VEGF stimulated VEGFR2 phosphorylation in lung tissues of nude mice in an exposure-dependent manner. Furthermore, elevation of FGF23 levels in plasma 24 hours post dosing suggests suppression of FGFR signaling. Sulfatinib demonstrates potent tumor growth inhibition in multiple human xenograft models and decreases CD31 expression remarkably, suggesting strong inhibition on angiogenesis through VEGFR and FGFR signaling. In a syngeneic murine colon cancer model CT-26, Sulfatinib demonstrates moderate tumor growth inhibition after single agent treatment[1]. After oral dosing of 10 mg/kg, the AUC and Cmax are 397 ng/mL and 138ng/mL in the mouse, 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.

Clinical Trial

分子量

480.58

Formula

C24H28N6O3S

CAS 号

1308672-74-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (208.08 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 2.0808 mL 10.4041 mL 20.8082 mL
5 mM 0.4162 mL 2.0808 mL 4.1616 mL
10 mM 0.2081 mL 1.0404 mL 2.0808 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。-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 (4.33 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.33 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 (4.33 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.33 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 (4.33 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.33 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]. PCT Int. Appl. (2011), WO 2011060746 A1 20110526.

Kinase Assay
[2]

The KDR kinase inhibition activity is tested using the the Z-lyte assay kit. The testing system contains 300 ng/mL of recombinant human KDR catalytic domain, 10 μM of ATP, 1 μM of substrate peptide, and a test compound (Sulfatinib) at a series of different concentrations in 384-well plate; total volume is 10 μL. The enzyme inhibition proceeds at room temperature (25°C), for 1 hour at room temperature on the shaker. 5 μL of stop solution is added to stop the reaction[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]

The phamacokinetics of Sulfatinib are studied with male ICR mice (n=6 for each group, weight 20-30g) after a single intraveneous and oral dosing at 2.5 and 10mg/kg, respectively. For i.v. dosing formulation, Sulfatinib is dissolved in DMSO (0.25%)-solutol(10%)-ethanol(10%)-physiological saline(79.75%) at the concentration of 0.25 mg/mL. And the p.o. Dosing formulation (1mg/mL) is prepared with 0.5% CMC-Na. After i.v. Or p.o. Dosing, blood samples are collected via the ophthalmic vein at 0 (pre-close), 5, 15, 30 min and 1, 1.5, 2, 4, 8, 24 h, anti-coagulated with heparin-Na. After centrifugation, plasma samples are seprated and protein precipitated with acetonitrilel containing internal standard[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]. PCT Int. Appl. (2011), WO 2011060746 A1 20110526.

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Sovleplenib(Synonyms: HMPL-523)

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。

Sovleplenib (Synonyms: HMPL-523)

Sovleplenib (HMPL-523) 是一种高效的、可口服的选择性 SYK 抑制剂,IC50 为 25 nM。具有抗肿瘤活性。Sovleplenib 可用于免疫性血小板减少症(ITP)的研究。

Sovleplenib(Synonyms: HMPL-523)

Sovleplenib Chemical Structure

CAS No. : 1415792-84-5

规格 价格 是否有货
5 mg ¥6800 询问价格 & 货期
10 mg ¥11000 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

Sovleplenib (HMPL-523) is a highly potent, orally available and selective SYK inhibitor with an IC50 of 25 nM. Anti-tumor activity. Sovleplenib can be used for the research of immune thrombocytopenia (ITP)[1].

IC50 & Target

SYK[1]

体外研究
(In Vitro)

Sovleplenib (HMPL-523) inhibits SYK, FLT3, KDR, LYN, FGFR2, and AUR A with IC50s of 0.025, 0.063, 0.390, 0.921, 3.214, 3.969 μM, respectively[1].
Sovleplenib (HMPL-523) blocks phosphorylation of BLNK, downstream protein of Syk, in human mantle cell line REC-1 and human plasma cell line ARH-7777 with IC50s of 0.105 µM and 0.173 μM, respectively[2].
Sovleplenib also inhibits cell viability of Ba/F3 Tel-Syk with the IC50 of 0.033 μM[2].
Sovleplenib also increases the apoptotic rate of REC-1 cells[2].
Sovleplenib shows the synergistic activities on killing human diffused large B cell lymphoma (DLBCL) in combination with other drugs such as BTK inhibitor, PI3Kδ inhibitors and Bcl2 family inhibitor[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)

Sovleplenib (HMPL-523) shows anti-tumor activity in vivo. Sovleplenib (100 mg/kg) inhibits tumor growth in REC-1 subcutaneous xenograft model[1].
Sovleplenib (HMPL-523; 100 mg/kg; daily oral administration) shows potent anti-tumor activity in B cell lymphoma REC-1 (TGI: 59%) in Syk dependent xenograft models [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 Model: Balb/c nude mice bearing subcutaneously implanted REC-1 cells or intravenously injected BA/F3 cells or BA/F3 TEL-SYK cells[1]
Dosage: 10 and 100 mg/kg
Administration: q.d.; for 8 days
Result: Inhibited tumor growth in REC-1 subcutaneous xenograft model at 100 mg/kg.

分子量

482.60

Formula

C24H30N6O3S

CAS 号

1415792-84-5

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]. Su WG, et al. Preparation of pyridopyrazine derivatives for use as Syk inhibitors. WO2012167733 A1.

    [2]. Na Yang, et al. HMPL-523, a Novel SYK Inhibitor Showed Anti-Tumor Activities In Vitro and In Vivo. Blood (2016) 128 (22): 3970.

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Amdizalisib(Synonyms: HMPL-689)

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。

Amdizalisib (Synonyms: HMPL-689)

Amdizalisib (HMPL-689) 是一种 PI3K 抑制剂,用于研究炎症、自身免疫性疾病或癌症。

Amdizalisib(Synonyms: HMPL-689)

Amdizalisib Chemical Structure

CAS No. : 1894229-05-0

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

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生物活性

Amdizalisib (HMPL-689) is a PI3K inhibitor and used for the research of inflammatory disease, autoimmune disease or cancer[1].

分子量

390.83

Formula

C19H15ClN8

CAS 号

1894229-05-0

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]. Su, Wei-Guo, et al.Preparation of imidazopyridazine compounds as PI3K inhibitors and their use.WO2016045591A1.

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Fruquintinib(Synonyms: 呋喹替尼; HMPL-013)

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。

Fruquintinib (Synonyms: 呋喹替尼; HMPL-013) 纯度: 99.94%

Fruquintinib (HMPL-013) 是有效,选择性的 VEGFR 1/2/3 抑制剂,IC50 值分别为33,0.5,and 35 nM。

Fruquintinib(Synonyms: 呋喹替尼; HMPL-013)

Fruquintinib Chemical Structure

CAS No. : 1194506-26-7

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 ¥1100 In-stock
5 mg ¥1000 In-stock
10 mg ¥1500 In-stock
50 mg ¥4500 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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  • Protein Tyrosine Kinase Compound Library
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  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • NMPA-Approved Drug Library
  • FDA Approved & Pharmacopeial Drug Library
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  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Targeted Therapy Drug Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Fruquintinib (HMPL-013) is a highly potent and selective VEGFR 1/2/3 inhibitor with IC50s of 33, 0.35, and 35 nM, respectively.

IC50 & Target[1]

VEGFR1

33 nM (IC50)

VEGFR2

35 nM (IC50)

VEGFR3

0.5 nM (IC50)

体外研究
(In Vitro)

Fruquintinib demonstrates potent inhibition on VEGF-A dependent KDR phosphorylation in HEK293-KDR cells and VEGF-A induced proliferation in primary HUVECs with IC50s of 0.6±0.2 nM and 1.7 nM, respectively. Similarly, potent VEGFR3 attenuation by fruquintinib is observed in primary HLECs, with IC50s of 1.5 nM and 4.2 nM for VEGF-C stimulated VEGFR3 phosphorylation and proliferation, respectively. Fruquintinib suppresses the tube branching, tube length and area in a concentration-dependent manner. The tubule length of primary HUVECs decreased by 74% and 94% at 0.03 and 0.3 μM of fruquintinib, respectively. Fruquintinib inhibits HUVEC tubule growth and CAM angiogenesis. Tube formation is suppressed significantly after treatment with fruquintinib at 0.3 μM for 18 hours[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)

Gastric cancer BGC-823 model is found to be most sensitive to fruquintinib. In this model, fruquintinib inhibits tumor growth by 62.3% and 95.4∼98.6%, at 0.5 and 2 mg/kg once daily dosing, respectively. When the dose is elevated to 5 mg/kg and 20 mg/kg, the tumors regress by 24.1% and 48.6%, respectively. The level of anti-tumor growth activity of fruquintinib varies in different tumor xenograft models. Fruquintinib significantly decreases the micro-vessel density even at the lowest dose of 0.8 mg/kg[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

393.39

Formula

C21H19N3O5

CAS 号

1194506-26-7

中文名称

呋喹替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 5.88 mg/mL (14.95 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5420 mL 12.7100 mL 25.4201 mL
5 mM 0.5084 mL 2.5420 mL 5.0840 mL
10 mM 0.2542 mL 1.2710 mL 2.5420 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。-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: ≥ 0.59 mg/mL (1.50 mM); Clear solution

    此方案可获得 ≥ 0.59 mg/mL (1.50 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 5.9 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: ≥ 0.59 mg/mL (1.50 mM); Clear solution

    此方案可获得 ≥ 0.59 mg/mL (1.50 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 5.9 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: ≥ 0.59 mg/mL (1.50 mM); Clear solution

    此方案可获得 ≥ 0.59 mg/mL (1.50 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 5.9 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]. Sun Q, et al. Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther. 2014;15(12):1635-45.

Cell Assay
[1]

Primary HUVECs or HLECs in exponential phase are suspended in 100 μL of RPMI-1640 media containing 0.5% FBS, and seeded at 5000 cell/well in 96-well plates pre-coated with 0.2% gelatin or fibronectin, and incubated overnight in a 5% CO2, 37°C incubator. Fruquintinib and VEGF-A165 or VEGF-C (50 ng/mL) are added and incubated for 48 hours. Viability of the cells is determined using CCK-8 assay format[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 Administration
[1]

Mice: The patient derived xenograft models are established after the primary tumor adopted serial passages in vivo. Once tumors have grown to 100-300 mm3, the animals are randomly assigned with 6-8 animals per group. The mice are treated orally with the vehicle (control group) or fruquintinib at a dose range of 0.5-20 mg/kg suspended in the vehicle (treated group) once daily for 3 weeks. In combination studies, docetaxel (Taxotere, 5 mg/kg) or oxaliplatin (10 mg/kg) is administered to nude mouse via intravenous injection, once a week. Tumor size and body weights are measured 3 times a week. Tumor volumes (TV) are calculated[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]. Sun Q, et al. Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther. 2014;15(12):1635-45.

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