Potent pan-Aurora kinase inhibitor
AMG 900 is a potent pan-Aurora kinase inhibitor (IC50 values are 1 nM, 4 nM, and 5 nM for Aurora C, B, and A, respectively). It is more than 10-fold selective for Aurora kinases over JNK2, Tie2, p38α, Met, and TYK2. AMG 900 inhibits autophosphorylation of Aurora A and B, as well as the phosphorylation of histone H3 on Ser in HeLa cells. AMG 900 inhibits proliferation of 26 tumor cell lines (EC50 ranges from 0.7 nM - 5.3 nM), including Paclitaxel (Cat. No. 1097)-resistant tumor cell lines. In an HCT116 tumor xenograft model, AMG 900 inhibits phosphorylation of histone H3 and tumor growth. It is orally bioavailable.
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-160785 |
| Réf. fabricant | 30000426 |
| Nom chimique ou matériau | N-[4-[[3-(2-Amino-4-pyrimidinyl)-2-pyridinyl]oxy]phenyl]-4-(4-methyl-2-thienyl)-1-phthalazinamine |
| CAS | 945595-80-2 |
| Quantité | 50 mg |
| Cible | Aurora Kinase Inhibitors |
| Formule moléculaire | C<sub>28</sub>H<sub>21</sub>N<sub>7</sub>OS |
| Pureté | 98% |
