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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Focal Adhesion Kinase (FAK)-VS-4718
VS-4718

Chemical Structure : VS-4718

CAS No.: 1061353-68-1

VS-4718 (PND-1186)

货号: PC-25664Not For Human Use, Lab Use Only.

VS-4718 (PND-1186) is a potent, highly-specific and reversible inhibitor of FAK with IC50 of 1.5 nM, promotes tumor cell apoptosis.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

VS-4718 (PND-1186) is a potent, highly-specific and reversible inhibitor of FAK with IC50 of 1.5 nM, promotes tumor cell apoptosis.
VS-4718 has an IC50 of ~100 nM in breast carcinoma cells as determined by anti-phospho-specific immunoblotting to FAK Tyr-397.
VS-4718 (0.1 uM) blocks FAK and p130Cas tyrosine phosphorylation, promotes caspase-3 activation, and triggers cell apoptosis.
VS-4718 inhibits 4T1 breast carcinoma subcutaneous tumor growth correlated with elevated tumor cell apoptosis and caspase 3 activation.
VS-4718 (150 mg/kg, oral) decreases tumor growth and spontaneous breast to lung metastasis in pre-clinical models.

物理化学性质&存储条件

分子量 501.51
分子式 C25H26F3N5O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-((2-((2-Methoxy-4-morpholinophenyl)amino)-5-(trifluoromethyl)pyridin-4-yl)amino)-N-methylbenzamide

参考文献

1. Tanjoni I, et al. Cancer Biol Ther. 2010 May 15;9(10):764-77.

2. Walsh C, et al. Cancer Biol Ther. 2010 May 15;9(10):778-90.

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