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Defactinib CAS: 1073154-85-4

Category: Inhibitors
Product Name: Defactinib
Cat No: I000337
CAS No: 1073154-85-4
Synonyms: N-methyl-4-[[4-[[3-[methyl(methylsulfonyl)amino]pyrazin-2-yl]methylamino]-5-(trifluoromethyl)pyrimidin-2-yl]amino]benzamide
Molecular Formula: C20H21F3N8O3S
Molecular Weight: 510.5
Solubility: DMSO: ≥ 39 mg/mL
Target: FAK
Storage: Store at -20°C
CAS 1073154-85-4,Defactinib
  • Description

Defactinib(VS-6063; PF-04554878) is a potent FAK phosphorylation inhibitor; overcomes YB-1–mediated paclitaxel
resistance by an AKT-dependent pathway.
IC50 value:
Target: FAK inhibitor
VS-6063 inhibited FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner. The combination of VS-6063 and paclitaxel markedly decreased proliferation and increased apoptosis, which resulted in 92.7% to 97.9% reductions in tumor weight. RPPA data showed that VS-6063 reduced levels of AKT and YB-1 in taxane-resistant cell lines. FAK inhibition enhanced chemosensitivity in taxane-resistant cells by decreasing YB-1 phosphorylation and subsequently CD44 in an AKT-dependent manner.

  • Spec

Appearance:A crystalline solid

  • References

[1]. Kang Y, et al. Role of focal adhesion kinase in regulating YB-1-mediated paclitaxel resistance in ovarian cancer. J Natl Cancer Inst. 2013 Oct 2;105(19):1485-95.

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