Inhibitor of mutant β-catenin signaling in hepatocellular carcinoma
WNTinib is a multi-kinase inhibitor with selectivity for mutant β-catenin (CTNNB1) in hepatocellular carcinoma compared to wild type hepatocytes (IC50 ranges are 0.36 μM-0.54 μM in primary organoids; 0.28 μM-1 μM in primary human HCC cell lines and 0.45 μM-2.3 μM in human cell lines ). Also inhibits VEGFR2, PDE6D and VEGFR1 (IC50 values are 0.3 μM, 0.3 μM and 0.6 μM respectively). Downregulates WNT and phospho-EZH2, upregulates trimethylation of H3K27 and normalises expression of apoptotic genes.
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-165685 |
| Réf. fabricant | 18794524 |
| Nom chimique ou matériau | 4-[3-Fluoro-4-[[[[4-(1,1,2,2,2-pentafluoroethyl)phenyl]amino]carbonyl]amino]phenoxy]-N-methyl-2-pyridinecarboxamide |
| CAS | 2770091-44-4 |
| Quantité | 10 mg |
| Cible | beta-Catenin |
| Formule moléculaire | C<sub>22</sub>H<sub>16</sub>F<sub>6</sub>N<sub>4</sub>O<sub>3</sub> |
| Pureté | 0.98 |
