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).
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-125871 |
| Réf. fabricant | 18718656 |
| Nom chimique ou matériau | N-Methyl-4-[[4-[[[3-[methyl(methylsulfonyl)amino]-2-pyrazinyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]benzamide |
| CAS | 1073154-85-4 |
| Quantité | 5 mg |
| Cible | Focal Adhesion Kinase Inhibitors |
| Formule moléculaire | C<sub>20</sub>H<sub>21</sub>F<sub>3</sub>N<sub>8</sub>O<sub>3</sub>S |
| Pureté | 0.98 |
