Chemical Name: N-Methyl-4-[[4-[[3-[methyl(methylsulfonyl)amino]pyrazin-2-yl]methylamino]-5-(trifluoromethyl)pyrimidin-2-yl]aminl]benzamide. Alternate Names: PF-04554878, VS-6063
FAK inhibitor
Molecular Weight:
510.50
Purity:
98% by HPLC NMR (Conforms)
Form:
White solid
CAS Number:
[1073154-85-4]
Formula:
C20H21F3N8O3S
Application Notes:
Defactinib (1073154-85-4) is a potent inhibitor of FAK (IC50 = 0.6nM) and Pyk2 (IC50 = 0.6nM).1 It is active in vivo (EC50 = 26nM). FAK inhibition prevents tumor invasion and dissemination rather than tumor size reduction. Defactinib has been shown to preferentially target cancer stem cells in a mouse xenograft model of triple negative breast cancer.2 It is in multiple clinical trials for various cancers3 and in shows synergistic activity when used in combination with checkpoint immunotherapy 4-6.
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