PF-04554878


CAS No. : 1073154-85-4

PF-04554878,1073154-85-4
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000337
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:510.49
Target:FAK
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Assay:≥98%
Appearance:A crystalline solid
Cat No:I000337
Cas No:1073154-85-4
Product-Name:PF-04554878
InChI:InChI=1S/C20H21F3N8O3S/c1-24-18(32)12-4-6-13(7-5-12)29-19-28-10-14(20(21,22)23)16(30-19)27-11-15-17(26-9-8-25-15)31(2)35(3,33)34/h4-10H,11H2,1-3H3,(H,24,32)(H2,27,28,29,30)
InChIKey:FWLMVFUGMHIOAA-UHFFFAOYSA-N
SMILES:CNC(=O)C1=CC=C(C=C1)NC2=NC=C(C(=N2)NCC3=NC=CN=C3N(C)S(=O)(=O)C)C(F)(F)F

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.


[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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