DATASHEET
Formulation
Pale yellow solid
Storage:
-20°C
Product Information:
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.
Description:
CAS Number: 1073154-85-4<br></br>Chemical Name: N-Methyl-4-[[4-[[3-[methyl(methylsulfonyl)amino]pyrazin-2-yl]methylamino]-5-(trifluoromethyl)pyrimidin-2-yl]aminl]benzamide<br></br>Molecular weight: 510.50<br></br>Formula: C20H21F3N8O3S<br></br>Solubility: DMSO (>25 mg/ml)<br></br>Physical Properties: White solid<br></br>Purity: 98% by HPLC NMR (Conforms)