S55746 hydrochloride(Synonyms: BCL201 hydrochloride)

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。

S55746 hydrochloride (Synonyms: BCL201 hydrochloride) 纯度: 98.69%

S55746 hydrochloride (BCL201 hydrochloride) 是一种有效、可口服、选择性的 BCL-2 抑制剂,其 Ki 值和 Kd 值分别为 1.3 nM 和 3.9 nM。S55746 hydrochloride (BCL201 hydrochloride) 具有抗肿瘤活性且毒性低。

S55746 hydrochloride(Synonyms: BCL201 hydrochloride)

S55746 hydrochloride Chemical Structure

CAS No. : 1448525-91-4

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S55746 hydrochloride 相关产品

相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Orally Active Compound Library
  • Anti-Blood Cancer Compound Library
  • Targeted Diversity Library

生物活性

S55746 hydrochloride (BCL201 hydrochloride) is a potent, orally active and selective BCL-2 inhibitor, with a Ki of 1.3 nM and a Kd of 3.9 nM. S55746 hydrochloride (BCL201 hydrochloride) has antitumor activity with low toxicity[1].

IC50 & Target[1]

Bcl-2

1.3 nM (Ki)

Bcl-xL

520 nM (Ki)

Bcl-2

3.9 nM (Kd)

Bcl-xL

186 nM (Kd)

体外研究
(In Vitro)

S55746 (0-1 μM) potently and selectively induces cell death[1].
S55746 selectively induces apoptosis through BCL-2 inhibition in a BAX/BAK-dependent manner[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.

Western Blot Analysis[1]

Cell Line: H146 and RS4;11 cell lines.
Concentration: 0, 0.1, 0.3 and 1 μM.
Incubation Time: 72 hours.
Result: Potently induced RS4;11 cell killing after 72 h of treatment with an IC50 of 71.6 nM.

体内研究
(In Vivo)

S55746 is a highly efficacious and well-tolerated (even at doses up to 300 mg/kg) orally active BCL-2 inhibitor [1].
S55746 (20-100 mg/kg, p.o.) inhibits xenograft growth in RS4;11 and Toledo models time- and dose-dependently[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: Female SCID/beige mice implanted subcutaneously with 3×106 Toledo or RS4;11[1].
Dosage: 20, 50, 100 mg/kg.
Administration: Oral gavage daily for 7 consecutive days.
Result: Induced significant anti-tumor activity time- and dose-dependently.
Animal Model: SCID/beige female mice with RS4;11 tumor xenografts[1].
Dosage: 25 and 100 mg/kg.
Administration: Single oral gavage treatment.
Result: Did not induce platelet loss in vivo at 25 and 100 mg/kg.

Clinical Trial

分子量

747.28

Formula

C43H43ClN4O6

CAS 号

1448525-91-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen

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

溶解性数据
In Vitro: 

DMSO : 200 mg/mL (267.64 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3382 mL 6.6909 mL 13.3819 mL
5 mM 0.2676 mL 1.3382 mL 2.6764 mL
10 mM 0.1338 mL 0.6691 mL 1.3382 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。

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    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 5 mg/mL (6.69 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (6.69 mM,饱和度未知) 的澄清溶液。

    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
  • 2.

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

    Solubility: ≥ 5 mg/mL (6.69 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (6.69 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]. Casara P, et al. S55746 is a novel orally active BCL-2 selective and potent inhibitor that impairs hematological tumor growth. Oncotarget. 2018 Apr 13;9(28):20075-20088.

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Bis-PEG2-PFP ester

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。

Bis-PEG2-PFP ester 

NH2-PEG3-BOC 是一种不可降解 (non-cleavable) 的含 2 个单元 PEG 的 ADC linker,可用于合成抗体偶联药物 (ADC)。Bis-PEG2-PFP ester 也是一种 PROTAC linker,属于 PEG 类。可用于合成 PROTAC 分子。

Bis-PEG2-PFP ester

Bis-PEG2-PFP ester Chemical Structure

CAS No. : 1314378-18-1

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生物活性

Bis-PEG2-PFP ester is also a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. Bis-PEG2-PFP ester is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[2].

IC50 & Target

PEGs

 

Alkyl/ether

 

Non-cleavable

 

体外研究
(In Vitro)

ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker[1].
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[2].

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

分子量

538.29

Formula

C20H12F10O6

CAS 号

1314378-18-1

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]. Matthew David DOROSKI, et al. Cytotoxic peptides and antibody drug conjugates thereof. WO2013072813A2.

    [2]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562.

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Aminooxy-PEG2-azide

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。

Aminooxy-PEG2-azide 

Aminooxy-PEG2-azide 是一种 PROTAC linker,属于 PEG 类,可用于合成 PROTAC 分子。Aminooxy-PEG2-azide 也是一种不可降解 (non-cleavable) 的含 2 个单元 PEG 的 ADC linker,可用于合成抗体偶联药物 (ADC)。

Aminooxy-PEG2-azide

Aminooxy-PEG2-azide Chemical Structure

CAS No. : 1043426-13-6

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生物活性

Aminooxy-PEG2-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. Aminooxy-PEG2-azide is also a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].

IC50 & Target[1][2]

PEGs

 

Non-cleavable

 

体外研究
(In Vitro)

PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker[2].

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

分子量

190.20

Formula

C6H14N4O3

CAS 号

1043426-13-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

参考文献
  • [1]. H. Tetsuo Uyeda, et al. Synthesis of surface ligands to prepare hydrophilic and biologically compatible quantum dots. doi: 10.1117/12.590494.

    [2]. Song, Ho Young, et al. Pyrrolobenzodiazepine dimer precursor and ligand-linker conjugate compound thereof.

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IACS-13909

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。

IACS-13909  纯度: 99.93%

IACS-13909 是一种有效的选择性的,具有口服活性的 SHP2 变构抑制剂,其 IC50 为 15.7 nM,Kd 为 32 nM。与其他磷酸酶 (包括 SHP1) 相比,IACS-13909 对 SHP2 的选择性更高。IACS-13909 抑制受体酪氨酸激酶 (RTK)/MAPK 途径的信号传导,并具有抗癌作用。

IACS-13909

IACS-13909 Chemical Structure

CAS No. : 2160546-07-4

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10 mM * 1 mL in DMSO ¥3300 In-stock
5 mg ¥3000 In-stock
10 mg ¥5000 In-stock
25 mg ¥10500 In-stock
50 mg   询价  
100 mg   询价  

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IACS-13909 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Orally Active Compound Library
  • Phosphatase Inhibitor Library

生物活性

IACS-13909 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC50 of 15.7 nM and a Kd of 32 nM. IACS-13909 is more selective for SHP2 than other phosphatases (including SHP1). IACS-13909 has antitumor activities and suppresses MAPK pathway signaling in receptor tyrosine kinases (RTK)-dependent cancers[1].

IC50 & Target

IC50: 15.7 nM (SHP2)[1]
Kd: 32 nM (SHP2)[1]

体外研究
(In Vitro)

IACS-13909 (10 nM-10 μM; 14 days) treatment potently suppresses the proliferation of wild-type SHP2 and KYSE-520 cells[1].
IACS-13909 (1-5 μM; 2 hours) treatment potently suppresses pERK and pMEK levels in wild-type SHP2 and KYSE-520 cells[1].
IACS-13909 potently suppresses the proliferation of both the parental cells and NCI-H1975 CS cells in a dose-dependent manner, with similar potency (GI50 ~1 μM). IACS-13909 (0.041-3.3 μM) suppresses pERK in NCI-H1975 CS cells in a dose-dependent manner[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 Proliferation Assay[1]

Cell Line: Wild-type SHP2 and KYSE-520 cells
Concentration: 10 nM, 100 nM, 1 μM, 10 μM
Incubation Time: 14 days
Result: Potently suppressed the cell proliferation.

Western Blot Analysis[1]

Cell Line: Wild-type SHP2 and KYSE-520 cells
Concentration: 1 μM, 5 μM
Incubation Time: 2 hours
Result: Potently suppressed pERK and pMEK levels.

体内研究
(In Vivo)

IACS-13909 (70 mg/kg; oral administration; daily; for 21 days) treatment potently suppresses tumor growth in mice, with 100% tumor growth inhibition (TGI) observed following 21 days of dosing[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: NSG mice (20-28 g) injected with KYSE-520 cells[1]
Dosage: 70 mg/kg
Administration: Oral administration; daily; for 21 days
Result: Potently suppressed tumor growth in mice.

分子量

377.27

Formula

C17H18Cl2N6

CAS 号

2160546-07-4

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 : 10 mg/mL (26.51 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6506 mL 13.2531 mL 26.5062 mL
5 mM 0.5301 mL 2.6506 mL 5.3012 mL
10 mM 0.2651 mL 1.3253 mL 2.6506 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: ≥ 1 mg/mL (2.65 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (2.65 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

*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]. Yuting Sun, et al. Allosteric SHP2 Inhibitor, IACS-13909, Overcomes EGFR-Dependent and EGFR-Independent Resistance Mechanisms toward Osimertinib. Cancer Res. 2020 Nov 1;80(21):4840-4853.

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Ribociclib-d6 hydrochloride(Synonyms: LEE011-d6 hydrochloride)

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。

Ribociclib-d6 hydrochloride (Synonyms: LEE011-d6 hydrochloride) 纯度: 98.37%

Ribociclib D6 (LEE011 D6) hydrochloride 是 Ribociclib 的一种氘代化合物。Ribociclib 是一种高度特异性的 CDK4/6 抑制剂,IC50 值分别为 10 nM 和 39 nM,对 cyclin B/CDK1 复合体的活性低于其 1000 倍。

Ribociclib-d6 hydrochloride(Synonyms: LEE011-d6 hydrochloride)

Ribociclib-d6 hydrochloride Chemical Structure

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5 mg ¥6500 In-stock
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生物活性

Ribociclib D6 (LEE011 D6) hydrochloride is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex[1].

分子量

477.04

Formula

C23H25D6ClN8O

中文名称

瑞博西尼盐酸盐 d6 (盐酸盐)

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)

参考文献
  • [1]. VanArsdale T, et al. Molecular Pathways: Targeting the Cyclin D-CDK4/6 Axis for Cancer Treatment. Clin Cancer Res. 2015 Jul 1;21(13):2905-10.

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Musk tibetene(Synonyms: Musk tibetine)

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。

Musk tibetene (Synonyms: Musk tibetine)

Musk tibetene (Musk tibetine) 是一种硝基麝香化合物,具有抗癌活性。Musk tibetine 在人淋巴细胞和人肝癌细胞系的微核试验中显示无基因毒性。

Musk tibetene(Synonyms: Musk tibetine)

Musk tibetene Chemical Structure

CAS No. : 145-39-1

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生物活性

Musk tibetene (Musk tibetine) is a nitro musk compound with carcinogenic activity. Musk tibetine reveals no genotoxicity in the micronucleus test with human lymphocytes and human hepatoma cell line[1][2].

体外研究
(In Vitro)

Musk tibetene reveals no genotoxicity in the micronucleus test with human lymphocytes and with the human hepatoma cell line Hep G2[1].
Musk tibetene reveals a cell-transforming potential that showed a dose-dependent response in our host-mediated assay system[2].

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

分子量

266.29

Formula

C13H18N2O4

CAS 号

145-39-1

中文名称

西藏麝香

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]. Kevekordes S, et al. Genotoxicity of nitro musks in the micronucleus test with human lymphocytes in vitro and the human hepatoma cell line Hep G2. Toxicol Lett. 1997 Mar 14;91(1):13-7.

    [2]. Apostolidis S, et al. Evaluation of carcinogenic potential of two nitro-musk derivatives, musk xylene and musk tibetene in a host-mediated in vivo/in vitro assay system. Anticancer Res. 2002 Sep-Oct;22(5):2657-62.

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MRTX0902

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。

MRTX0902 

MRTX0902 是一种有效的 SOS1 的抑制剂,IC50 为 46 nM。

MRTX0902

MRTX0902 Chemical Structure

CAS No. : 2654743-22-1

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5 mg ¥9500 询问价格 & 货期
10 mg ¥15000 询问价格 & 货期

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生物活性

MRTX0902 is a potent SOS1 inhibitor with an IC50 of 46 nM (WO2021127429A1; Example 12-10)[1].

IC50 & Target[1]

KRAS-SOS1

46 nM (IC50)

分子量

388.47

Formula

C22H24N6O

CAS 号

2654743-22-1

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]. Matthew Arnold Marx, et al. Sos1 inhibitors. WO2021127429A1.

    [2]. Matthew Arnold Marx, et al. Sos1 inhibitors. WO2021127429A1.

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Aminooxy-PEG4-alcohol

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。

Aminooxy-PEG4-alcohol 

Aminooxy-PEG4-alcohol 是一种不可降解 (non-cleavable) 的含 4 个单元 PEG 的 ADC linker,可用于合成抗体偶联药物 (ADC)。Aminooxy-PEG4-alcohol 也是一种 PROTAC linker,属于 PEG 类,可用于合成 PROTAC 分子。

Aminooxy-PEG4-alcohol

Aminooxy-PEG4-alcohol Chemical Structure

CAS No. : 106492-60-8

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生物活性

Aminooxy-PEG4-alcohol is a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. Aminooxy-PEG4-alcohol is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[2].

IC50 & Target[1][2]

PEGs

 

Non-cleavable

 

体外研究
(In Vitro)

ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker[1].
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[2].

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

分子量

209.24

Formula

C8H19NO5

CAS 号

106492-60-8

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]. Heather D. Maynard, et al. Method of creating hydrogels through oxime bond formation. US20150202305A1.

    [2]. Murray BS, et al. Reactive thermoresponsive copolymer scaffolds. Chem Commun (Camb). 2010 Dec 7;46(45):8651-3.

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Pilaralisib analogue(Synonyms: XL147 analogue)

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。

Pilaralisib analogue (Synonyms: XL147 analogue) 纯度: 99.67%

Pilaralisib analogue (XL147 analogue) 是一种代表性的选择性 PI3Kα 抑制剂,详细信息请参考专利文献 WO2012006552A1 中 Table 1 中的化合物 147。

Pilaralisib analogue(Synonyms: XL147 analogue)

Pilaralisib analogue Chemical Structure

CAS No. : 956958-53-5

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生物活性

Pilaralisib analogue (XL147 analogue) is a representative and selective PI3Kα inhibitor extracted from patent WO2012006552A1, Compound 147 in Table 1.

IC50 & Target[1]

PI3K-alpha

 

分子量

448.52

Formula

C21H16N6O2S2

CAS 号

956958-53-5

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 : ≥ 50 mg/mL (111.48 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 2.2296 mL 11.1478 mL 22.2956 mL
5 mM 0.4459 mL 2.2296 mL 4.4591 mL
10 mM 0.2230 mL 1.1148 mL 2.2296 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: ≥ 2.5 mg/mL (5.57 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.57 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 (5.57 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.57 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 (5.57 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.57 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]. Carlos L. Arteaga, et al. Combinations of kinase inhibitors for the treatment of cancer. WO 2012006552 A1.

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Aminooxy-PEG1-azide

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。

Aminooxy-PEG1-azide 

Aminooxy-PEG1-azide 是一种 PROTAC linker,属于 PEG 类,可用于合成 PROTAC。

Aminooxy-PEG1-azide

Aminooxy-PEG1-azide Chemical Structure

CAS No. : 2100306-70-3

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生物活性

Aminooxy-PEG1-azide is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].

IC50 & Target[1]

PEGs

 

体外研究
(In Vitro)

PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

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

分子量

146.15

Formula

C4H10N4O2

CAS 号

2100306-70-3

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]. Zhang F, et al. Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. Bioorg Med Chem. 2020 Jan 1;28(1):115228.

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R1530

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。

R1530  纯度: 99.06%

R1530 是一种高效的,具有口服活性的有丝分裂/血管生成 (mitosis/angiogenesis) 双重作用抑制剂,具有抗肿瘤和抗血管生成活性。R1530 是一种多激酶抑制剂,与 31 种激酶结合的 Kd 均小于 500 nM。R1530 抑制 VGFR2FGFR1 作用的 IC50 分别为 10 nM 和 28 nM。

R1530

R1530 Chemical Structure

CAS No. : 882531-87-5

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生物活性

R1530 is a highly potent, orally active, dual-acting mitosis/angiogenesis inhibitor, with anti-tumor and anti-angiogenic activities. R1530 is a multikinase inhibitor which binds to 31 kinases with Kds of <500 nm. r1530 inhibits VGFR2 and FGFR1 with IC50s of 10 nM and 28 nM, respectively[1][2][3].

IC50 & Target[1]

KDR

10 nM (IC50)

FGFR1

28 nM (IC50)

分子量

356.78

Formula

C18H14ClFN4O

CAS 号

882531-87-5

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 : 2 mg/mL (5.61 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8028 mL 14.0142 mL 28.0285 mL
5 mM 0.5606 mL 2.8028 mL 5.6057 mL
10 mM

*

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。

参考文献
  • [1]. Jin-Jun Liu, et al. Discovery of a Highly Potent, Orally Active Mitosis/Angiogenesis Inhibitor R1530 for the Treatment of Solid Tumors. ACS Med Chem Lett. 2013 Feb 14; 4(2): 259–263.

    [2]. Christian Tovar, et al. Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy. Cell Cycle. 2010 Aug 15;9(16):3364-75.

    [3]. Kolinsky K, et al. Preclinical evaluation of the novel multi-targeted agent R1530. Cancer Chemother Pharmacol. 2011 Dec;68(6):1585-94.

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Aminooxy-PEG3-azide

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。

Aminooxy-PEG3-azide 

Aminooxy-PEG3-azide 是一种不可降解 (non-cleavable) 的含 3 个单元 PEG 的 ADC linker,可用于合成抗体偶联药物 (ADC)。Aminooxy-PEG3-azide 也是一种 PROTAC linker,属于 PEG 类,可用于合成 PROTAC 分子。

Aminooxy-PEG3-azide

Aminooxy-PEG3-azide Chemical Structure

CAS No. : 1306615-51-9

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

Aminooxy-PEG3-azide is a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. Aminooxy-C2-PEG3-azide is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[2].

IC50 & Target[1][2]

PEGs

 

Non-cleavable

 

体外研究
(In Vitro)

ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker[1].
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[2].

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

分子量

234.25

Formula

C8H18N4O4

CAS 号

1306615-51-9

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]. Chanhyuk KIM, et al. Optimized chimeric receptor t cell switches and uses thereof. WO2016168766A1.

    [2]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562.

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BAMB-4(Synonyms: ITPKA-IN-C14)

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。

BAMB-4 (Synonyms: ITPKA-IN-C14) 纯度: 99.99%

BAMB-4(ITPKA-IN-C14)是新型的膜渗透型ITPKA抑制剂,在ADP-Glo实验中IC50为37uM。

BAMB-4(Synonyms: ITPKA-IN-C14)

BAMB-4 Chemical Structure

CAS No. : 891025-25-5

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3237 In-stock
2 mg ¥2333 In-stock
5 mg ¥3500 In-stock
10 mg ¥5000 In-stock
50 mg   询价  
100 mg   询价  

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生物活性

BAMB-4(ITPKA-IN-C14) is a new membrane-permeable inhibitor against inositol-1,4,5-trisphosphate-3-kinase A((ITPKA) with IC50 of 37 μM in ADP-Glo Assay. IC50 value: 37 uM Target: ITPKA inhibitor BAMB-4 exhibit the lowest inhibition frequency among the InsP3- Kinase inhibitors. only in one from 42 targets tested, BAMB-4 showed an inhibitory effect. Noteworthy, in kinase screens no targets of BAMB-4 were detected, indicating that the compound does not belong to the typical kinase inhibitors. Thus, the relative high specificity and the high cellular uptake of BAMB-4 now for the rst provide the possibility to effectively inhibit InsP3kinase in vivo. e InsP3Kinase activity is essentially involved in ITPKA promoted metastasis of lung cancer cells, BAMB-4 is a promising therapeutic approach in lung cancer therapy.

分子量

252.27

Formula

C15H12N2O2

CAS 号

891025-25-5

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 : ≥ 40 mg/mL (158.56 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 3.9640 mL 19.8200 mL 39.6401 mL
5 mM 0.7928 mL 3.9640 mL 7.9280 mL
10 mM 0.3964 mL 1.9820 mL 3.9640 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。

参考文献
  • [1]. Schroder D, et al. Identification of a new membrane-permeable inhibitor against inositol-1,4,5-trisphosphate-3-kinase A. Biochem Biophys Res Commun. 2013 Sep 20;439(2):228-34.

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Aminooxy-PEG4-azide

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。

Aminooxy-PEG4-azide 

Aminooxy-PEG4-azide 是一种 PROTAC linker,属于 PEG 类,可用于合成 PROTAC。

Aminooxy-PEG4-azide

Aminooxy-PEG4-azide Chemical Structure

CAS No. : 2100306-61-2

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

* Please select Quantity before adding items.

生物活性

Aminooxy-PEG4-azide is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].

IC50 & Target[1]

PEGs

 

体外研究
(In Vitro)

PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

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

分子量

278.31

Formula

C10H22N4O5

CAS 号

2100306-61-2

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]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562.

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Ombrabulin hydrochloride(Synonyms: AVE8062 hydrochloride; AC7700 hydrochloride)

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。

Ombrabulin hydrochloride (Synonyms: AVE8062 hydrochloride; AC7700 hydrochloride) 纯度: 99.84%

Ombrabulin hydrochloride 是 CA-4 磷酸酯的衍生物,选择性破坏内皮细胞的微管蛋白细胞骨架,具有抗血管作用。

Ombrabulin hydrochloride(Synonyms: AVE8062 hydrochloride; AC7700 hydrochloride)

Ombrabulin hydrochloride Chemical Structure

CAS No. : 253426-24-3

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10 mM * 1 mL in Water ¥1100 In-stock
5 mg ¥1000 In-stock
10 mg ¥1600 In-stock
25 mg ¥3500 In-stock
50 mg ¥5600 询价
100 mg ¥8900 询价
200 mg   询价  
500 mg   询价  

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  • Anti-Lung Cancer Compound Library
  • Rare Diseases Drug Library

生物活性

Ombrabulin hydrochloride is a derivative of CA-4 phosphate, which is known to exhibit antivascular effects through selective disruption of the tubulin cytoskeleton of endothelial cells.

IC50 & Target

tubulin[1]

体外研究
(In Vitro)

The effect of Ombrabulin (AVE8062) on endothelial or tumor cell viability is examined using the MTT assay. The IC50 of Ombrabulin for the mouse mesenteric endothelial cells (MMEC) is 10 nM and ranges between 7 and 20 nM for the tumor cell lines (HeyA8, SKOV3ip1, and HeyA8-MDR). Comparative analysis of the nonlinear least-squares regression of the dose-response curves for each agent alone and combination Ombrabulin /Docetaxel show a significantly lower IC50 than either agent alone (P<0.005, all cell lines). The cytotoxicity of Docetaxel is 2- to 4-fold greater in combination with Ombrabulin for the endothelial and tumor cells compared with Docetaxel alone[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)

Before performing therapy experiments, the tolerability of various doses of Ombrabulin (AVE8062) ranging from 10 to 100 mg/kg is tested given twice weekly via i.v., i.p., or s.c. routes in nude mice (n=3 per group). The i.v. and s.c. routes are not pursued further due to problems with skin or tail vein necrosis. The i.p. route is well tolerated with doses up to 100 mg/kg. Next, preliminary experiments are done to determine the lowest dose for in vivo therapeutic efficacy. Starting 7 days after tumor cell injection, nude mice (n=5 per group) bearing HeyA8 ovarian cancer cells are treated with either vehicle or Ombrabulin 10, 30, 50, and 100 mg/kg twice weekly i.p. for 3 weeks. There is 65% reduction in tumor weight in the 30 mg/kg group compared with the vehicle control group (P<0.02). The 10 mg/kg dose is not effective. The antitumor effects at doses >30 mg/kg are not significantly better; therefore, the 30 mg/kg dose is selected for subsequent therapy experiments[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

438.90

Formula

C21H27ClN2O6

CAS 号

253426-24-3

中文名称

奥瑞布林盐酸盐

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: 

H2O : 20 mg/mL (45.57 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2784 mL 11.3921 mL 22.7842 mL
5 mM 0.4557 mL 2.2784 mL 4.5568 mL
10 mM 0.2278 mL 1.1392 mL 2.2784 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]. Kim TJ, et al. Antitumor and antivascular effects of AVE8062 in ovarian carcinoma. Cancer Res. 2007 Oct 1;67(19):9337-45.

Cell Assay
[1]

The capacity of Ombrabulin (AVE8062) to modulate MMEC and HeyA8 cell cycle as well as apoptosis is analyzed by flow cytometry. In all assays, 3×106 tumor cells are seeded into Petri dishes and allowed to adhere overnight. The cultures are then washed with PBS and treated with regular medium (negative control) or medium containing Docetaxel, Ombrabulin (HeyA8, 20 nM; MMEC 10 nM), or Ombrabulin plus Docetaxel. For cell cycle analyses, tumor cells are collected by trypsinization and pooled with the cells floating in the medium. The cell suspensions are centrifuged for 5 min at 1,500 rpm at room temperature, then washed and fixed with ethanol. For apoptosis analysis, cells are incubated overnight in 50 μL of DNA labeling solution (10 μL of reaction buffer, 0.75 μL of TdT enzyme, 8 μL of FITC-dUTP, and 32.25 μL of distilled water) at room temperature. Following the addition of rinse buffer, samples are centrifuged, washed, and fixed in ethanol. All samples are then washed with PBS, then resuspended in propidium iodide (50 μg/mL) and RNase A (20 μg/mL) in PBS for 30 min at room temperature. Stained cells are analyzed on an EPICS XL flow cytometer. The low-level gate is set at the base of the G1 peak and the percentages of cells within the G1 and G2-M phases of the cell cycle are determined by analysis with Multicycle[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[1]
Female athymic nude mice (6-8 weeks old) are used. For in vivo injection, tumor cells are trypsinized, centrifuged at 1,000 rpm ×7 min at 4°C, washed twice, and resuspended in serum-free HBSS at a concentration of 5×106 cells/mL (SKOV3ip1 and HeyA8-MDR) and 1.25×106 cells/mL (HeyA8). Tumors are established by i.p. injection of cells. Ombrabulin therapy is initiated 7 or 17 days after cell line injection. Mice (n=10 per group) are randomly assigned to the following treatment groups: (a) PBS 200 μL, i.p. weekly; (b) Ombrabulin 30 mg/kg [dissolved in PBS (pH 5)] i.p. twice weekly; (c) Docetaxel 2 mg/kg (HeyA8 and HeyA8-MDR) or 1.4 mg/kg (SKOV3ip1) i.p. weekly; (d) Ombrabulin plus Docetaxel (both drugs given at the doses and frequency described above for each drug alone). The dose of Ombrabulin used in these experiments is optimized from dose-escalation studies against tumor growth. Mice are monitored for signs of adverse effects and tumors are harvested after treatment (range 2-5 weeks). The mouse weight, tumor weight, number of tumor nodules, and volume of ascites are recorded at necropsy.

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]. Kim TJ, et al. Antitumor and antivascular effects of AVE8062 in ovarian carcinoma. Cancer Res. 2007 Oct 1;67(19):9337-45.

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Aminooxy-PEG2-alcohol

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。

Aminooxy-PEG2-alcohol 

Aminooxy-PEG2-alcohol 是一种不可降解 (non-cleavable) 的含 2 个单元 PEG 的 ADC linker,可用于合成抗体偶联药物 (ADC)。Aminooxy-PEG2-alcohol 也是一种 PROTAC linker,属于 PEG 类,可用于合成 PROTAC 分子。

Aminooxy-PEG2-alcohol

Aminooxy-PEG2-alcohol Chemical Structure

CAS No. : 185022-12-2

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

* Please select Quantity before adding items.

生物活性

Aminooxy-PEG2-alcohol is a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. Aminooxy-PEG2-alcohol is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[2].

IC50 & Target[1][2]

PEGs

 

Non-cleavable

 

体外研究
(In Vitro)

ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker[1].
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[2].

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

分子量

121.14

Formula

C4H11NO3

CAS 号

185022-12-2

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]. Marek Kwiatkowski. Conjugates of biologically active molecules to functionalized polymers. WO2013186632A2.

    [2]. Murray BS, et al. Reactive thermoresponsive copolymer scaffolds. Chem Commun (Camb). 2010 Dec 7;46(45):8651-3.

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ILK-IN-2(Synonyms: OSU-T315 analog)

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。

ILK-IN-2 (Synonyms: OSU-T315 analog) 纯度: 98.14%

ILK-IN-2 (OSU-T315 analog) 是一种ILK抑制剂。

ILK-IN-2(Synonyms: OSU-T315 analog)

ILK-IN-2 Chemical Structure

CAS No. : 1333146-24-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2817 In-stock
2 mg ¥1200 In-stock
5 mg ¥2400 In-stock
50 mg ¥4100 询价
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

ILK-IN-2 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Cytoskeleton Compound Library

生物活性

ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor.

分子量

533.59

Formula

C30H30F3N5O

CAS 号

1333146-24-9

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 : 50 mg/mL (93.70 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8741 mL 9.3705 mL 18.7410 mL
5 mM 0.3748 mL 1.8741 mL 3.7482 mL
10 mM 0.1874 mL 0.9370 mL 1.8741 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: ≥ 5 mg/mL (9.37 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (9.37 mM,饱和度未知) 的澄清溶液。

    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% corn oil

    Solubility: ≥ 5 mg/mL (9.37 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (9.37 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。

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

Propargyl-PEG5-amine

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。

Propargyl-PEG5-amine  纯度: ≥95.0%

Propargyl-PEG5-amine 是一种不可降解 (non-cleavable) 的 ADC linker,用于抗体偶联药物 (ADCs) 的合成。Propargyl-PEG5-amine 是一种 PROTAC linker,属于 PEG 类。Propargyl-PEG5-NH2 可用于合成一系列 PROTAC 分子。

Propargyl-PEG5-amine

Propargyl-PEG5-amine Chemical Structure

CAS No. : 1589522-46-2

规格 价格 是否有货 数量
25 mg ¥800 In-stock
50 mg ¥1300 In-stock
100 mg ¥2000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Propargyl-PEG5-amine is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Propargyl-PEG5-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].

IC50 & Target[1]

Non-cleavable

 

PEGs

 

体外研究
(In Vitro)

ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker.PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.

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

分子量

275.34

Formula

C13H25NO5

CAS 号

1589522-46-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL (363.19 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6319 mL 18.1594 mL 36.3187 mL
5 mM 0.7264 mL 3.6319 mL 7.2637 mL
10 mM 0.3632 mL 1.8159 mL 3.6319 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 (protect from 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: ≥ 2.5 mg/mL (9.08 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.08 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 (9.08 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.08 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 (9.08 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.08 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]. Robert Zamboni, et al. Raf-degrading conjugate compounds. WO2018200981A1.

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

CAY10505

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。

CAY10505  纯度: 99.75%

CAY10505 是一种有效的选择性 PI3Kγ 抑制剂,作用于神经元细胞,IC50 为 30 nM。

CAY10505

CAY10505 Chemical Structure

CAS No. : 1218777-13-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥500 In-stock
10 mg ¥420 In-stock
25 mg ¥750 In-stock
50 mg ¥1300 In-stock
100 mg ¥2100 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

CAY10505 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Kinase Inhibitor Library
  • PI3K/Akt/mTOR Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Differentiation Inducing Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Angiogenesis Related Compound Library
  • Glucose Metabolism Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

CAY10505 is a potent and selective PI3Kγ inhibitor with an IC50 of 30 nM in neurons.

IC50 & Target[1]

PI3Kγ

30 nM (IC50, Neurons)

体外研究
(In Vitro)

A class IB PI3Kγ isoform inhibitor CAY10505 at 200 nM (IC50=30 nM) partially reduces the baicalein-induced Akt phosphorylation in neurons[1]. The pharmacological PI3K inhibitor CAY10505 (PIK3CG) is tested on an extended panel of multiple myeloma (MM) cell lines and freshly isolated primary MM samples. MM cells are CAY10505-treated for 3 d (MM cell lines) or 5 d (primary MM cells) respectively, and survival is analysed by flow cytometry (annexin V-FITC/PI staining). Treatment of bone marrow stromal cells (BMSCs)-co-cultured primary MM samples with the PIK3CA inhibitor CAY10505 results in anti-survival effects (mean survival relative to DMSO-treated controls: CAY10505: 84±14%, tested at 10 μM)[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)

Administration of CAY10505 (0.6 mg/kg, p.o.), Losartan (25 mg/kg, p.o.), or Atorvastatin (30 mg/kg, p.o.) significantly increases serum nitrite and (or) nitrate concentrations in hypertensive rats. Acetylcholine (ACh) and Sodium nitroprusside (SNP) produce endothelium-dependent and-independent relaxation in isolated rat aortic ring precontracted with Phenylephrine (3 μM), in a dose dependent manner. Administration of CAY10505 (0.6 mg/kg,p.o.), Losartan (25 mg/kg, p.o.), or Atorvastatin (30 mg/kg, p.o.) significantly prevents hypertension-induced attenuation of ACh-induced endothelium-dependent relaxation. Deoxycorticosterone acetate salt (DOCA, 40 mg/kg, s.c.) induced hypertension markedly attenuates acetylcholine-induced endothelium-dependent relaxation, but does not affect SNP-induced endotheliumindependent relaxation[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.

分子量

289.28

Formula

C14H8FNO3S

CAS 号

1218777-13-9

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 : ≥ 34 mg/mL (117.53 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 3.4569 mL 17.2843 mL 34.5686 mL
5 mM 0.6914 mL 3.4569 mL 6.9137 mL
10 mM 0.3457 mL 1.7284 mL 3.4569 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。

参考文献
  • [1]. Sun YY, Lin SH et al. Cell type-specific dependency on the PI3K/Akt signaling pathway for the endogenous Epo and VEGF induction by baicalein in neurons versus astrocytes. 2013 Jul 19;8(7):e69019.

    [2]. Tyagi S. Effect of phosphatidylinositol 3-kinase-γ inhibitor CAY10505 in hypertension, and its associated vascular endothelium dysfunction in rats. Can J Physiol Pharmacol. 2012 Jul, 90(7), 881-5.

    [3]. Hofmann C, et al. PI3K-dependent multiple myeloma cell survival is mediated by the PIK3CA isoform. Br J Haematol. 2014 Aug;166(4):529-39.

    [4]. Jingyi Wang, et al. MiR-1976 Knockdown Promotes Epithelial-Mesenchymal Transition and Cancer Stem Cell Properties Inducing Triple-Negative Breast Cancer Metastasis. Cell Death Dis. 2020 Jul 3;11(7):500.

Cell Assay
[2]

Up to 5×104 multiple myeloma (MM) cells/100 μL of medium per well are seeded in 96-well-plates. Primary MM cells are always seeded into wells containing primary bone marrow stromal cells. Drugs (e.g., CAY10505) are dissolved in either DMSO or acidified ethanol (in the case of melphalan) and kept as frozen stock solutions of 10-50 mM. Working dilutions in fullmedium are always freshly prepared. In the case of Bortezomib small volumes of single-thaw stock solution aliquots are prepared. Drug dilutions (e.g., CAY10505, 2.5, 5, 7.5 and 10 μM) are added to MM cells as 100 μL of 2× the final concentration per well for single-drug treatments, and in appropriate volumes of higher concentrations for drug combinations. Solvent controls are always included[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]

Rats[3]
Wistar albino rats (180-240 g) of either sex are employed in the present study. For each group, the number of rats used (n) is 6. Group I (normal control): Rats are maintained on a diet of normal chow with drinking water. Group II (hypertensive control): Rats are unilaterally nephrectomized (uninephrectomised) and DOCA (40 mg/kg) is administered by subcutaneous injection (s.c.) twice weekly for 6 weeks, and then the untreated drinking water is replaced with a 1% NaCl solution. Group III (hypertensive rats): Rats are treated with CAY10505 (0.6 mg/kg, per os (p.o)) for 1 week after 5 weeks of treatment with DOCA. Group IV (hypertensive rats): Rats are treated with Losartan (25 mg/kg, p.o.) for 1 week after 5 weeks of treatment with DOCA. Group V (hypertensive rats): Rats are treated with Atorvastatin (30 mg/kg, p.o.) for 1 week after 5 weeks of treatment with DOCA.

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 YY, Lin SH et al. Cell type-specific dependency on the PI3K/Akt signaling pathway for the endogenous Epo and VEGF induction by baicalein in neurons versus astrocytes. 2013 Jul 19;8(7):e69019.

    [2]. Tyagi S. Effect of phosphatidylinositol 3-kinase-γ inhibitor CAY10505 in hypertension, and its associated vascular endothelium dysfunction in rats. Can J Physiol Pharmacol. 2012 Jul, 90(7), 881-5.

    [3]. Hofmann C, et al. PI3K-dependent multiple myeloma cell survival is mediated by the PIK3CA isoform. Br J Haematol. 2014 Aug;166(4):529-39.

    [4]. Jingyi Wang, et al. MiR-1976 Knockdown Promotes Epithelial-Mesenchymal Transition and Cancer Stem Cell Properties Inducing Triple-Negative Breast Cancer Metastasis. Cell Death Dis. 2020 Jul 3;11(7):500.

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Bis-PEG3-PFP ester

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。

Bis-PEG3-PFP ester 

Bis-PEG3-PFP ester 是一种 PROTAC linker,属于 PEG 类。可用于合成 PROTAC 分子。

Bis-PEG3-PFP ester

Bis-PEG3-PFP ester Chemical Structure

CAS No. : 1314378-13-6

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生物活性

Bis-PEG3-PFP ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

IC50 & Target

PEGs

 

Alkyl/ether

 

体外研究
(In Vitro)

PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

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

分子量

582.34

Formula

C22H16F10O7

CAS 号

1314378-13-6

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]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562.

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