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Defactinib

Overview
Catalog # bs-83039c-5-mg
Product Name Defactinib
Specifications
Storage Buffer Pale yellow solid
Storage Condition -20°C
Target
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

Chemical Name: N-Methyl-4-[[4-[[3-[methyl(methylsulfonyl)amino]pyrazin-2-yl]methylamino]-5-(trifluoromethyl)pyrimidin-2-yl]aminl]benzamide

Molecular weight: 510.50

Formula: C20H21F3N8O3S

Solubility: DMSO (>25 mg/ml)

Physical Properties: White solid

Purity: 98% by HPLC NMR (Conforms)