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

Chemical Structure : Defactinib hydrochloride

CAS No.: 1073160-26-5

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Defactinib hydrochloride (VS-6063;VS6063;PF04554878;PF-04554878)

货号: PC-42952Not For Human Use, Lab Use Only.

Defactinib (VS-6063,PF-04554878) is a potent, selective and orally active FAK inhibitor, inhibits pFAK (Tyr397) in a dose-dependent manner in cancer cell lines.

规格 价格 库存 数量
10 mg ￥980 In stock
25 mg ￥1580 In stock
50 mg ￥2480 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Defactinib (VS-6063,PF-04554878) hydrochloride is a potent, selective and orally active FAK inhibitor, inhibits pFAK (Tyr397) in a dose-dependent manner in cancer cell lines.
Defactinib shows no statistically significant changes in FAK phosphorylation at the other residues(Tyr 576/577, Tyr 925, or Tyr 861), also inhibits Pyk2 Tyr402 phosphorylation in HeyA8 cells.
Defactinib markedly decreases proliferation and increases apoptosis combined with paclitaxel, reduces levels of AKT and YB-1 in taxane-resistant cell lines.
Defactinib significantly reduces tumor growth, synergized with the mTOR inhibitor everolimus in xenograft models of pancreatic tumor.

物理化学性质&存储条件

分子量 546.9537
分子式 C20H22ClF3N8O3S
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

Benzamide, N-methyl-4-[[4-[[[3-[methyl(methylsulfonyl)amino]-2-pyrazinyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-, hydrochloride (1:1)

参考文献

1. Kang Y, et al. J Natl Cancer Inst. 2013 Oct 2;105(19):1485-95.

2. Shimizu T, et al. Cancer Chemother Pharmacol. 2016 May;77(5):997-1003.

3. Jones SF, et al. Invest New Drugs. 2015 Oct;33(5):1100-7.

4. François RA, et al. J Natl Cancer Inst. 2015 May 12;107(8). pii: djv123.

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