Chemical Structure : Defactinib hydrochloride
CAS No.: 1073160-26-5
Catalog No.: 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.
Packing | Price | Stock | Quantity |
---|---|---|---|
10 mg | $98 | In stock | |
25 mg | $158 | In stock | |
50 mg | $248 | In stock | |
100 mg | Get quote |
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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.
M.Wt | 546.9537 | |
Formula | C20H22ClF3N8O3S | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
Benzamide, N-methyl-4-[[4-[[[3-[methyl(methylsulfonyl)amino]-2-pyrazinyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-, hydrochloride (1:1) |
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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