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Tocris Bioscience™ Defactinib
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Catalog No. 730525
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Quantity:
5 mg
25 mg
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This item is not returnable. View return policy

Potent and selective FAK and Pyk2 inhibitor

Defactinib is a potent and selective focal adhesion kinase (FAK) and proline rich tyrosine kinase 2 (Pyk2) inhibitor (IC50 = 0.6 nM at both). The compound shows >100-fold selectivity for FAK and Pyk2 over other kinases. Defactinib inhibits FAK phosphorylation in vivo (EC50 = 26 nM), and inhibits tumor growth. Defactinib also decreases the viability of thyroid cancer cells, showing greater selectivity for TT and K1 cells compared to FAK Inhibitor 14 (Cat. No. 3414) (IC50 values are 1.98 μM and 10.34 μM, respectively). Defactinib suppresses colony growth of Pnf cells when combined with Selumetinib (Cat. No. 6815).

Specifications

Chemical Name or Material N-Methyl-4-[[4-[[[3-[methyl(methylsulfonyl)amino]-2-pyrazinyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]benzamide
CAS 1073154-85-4
Quantity 25 mg
Target Focal Adhesion Kinase Inhibitors
Molecular Formula C20H21F3N8O3S
Purity 0.98
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