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Chemical Structure : Defactinib
CAS No.: 1073154-85-4
Catalog No.: PC-42951Not For Human Use, Lab Use Only.
Defactinib (VS-6063, PF-04554878) is a potent, selective and orally active FAK inhibitor, selectively inhibits pFAK (Tyr397) in a dose-dependent manner in cancer cell lines.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $148 | In stock | |
| 50 mg | $208 | In stock | |
| 100 mg | $288 | In stock | |
| 500 mg | $678 | In stock | |
| 1 g | Get quote | ||
| 5 g | Get quote |
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Defactinib (VS-6063, PF-04554878) is a potent, selective and orally active FAK inhibitor, selectively 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 | 510.4927 | |
| Formula | C20H21F3N8O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: ≥ 39 mg/mL |
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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]- |
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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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