Potent and selective Wee1 inhibitor
Adavosertib is a potent and selective Wee1 inhibitor (IC50 = 5.2 nM). In a panel of 223 serine/threonine or tyrosine kinases, Adavosertib is highly selective for Wee 1 over all except 8 kinases. In particular Adavosertib shows >100-fold selectivity over human Myt1. Adavosertib blocks CDC2Y15 phosphorylation and Gemcitabine (Cat. No. 3259)-induced DNA damage checkpoint, leading to premature mitotic entry and apoptosis in p53-deficient tumor cell lines. Adavosertib also potentiates the cytotoxic effects of Pemetrexed (Cat. No. 6185), Doxorubicin (Cat. No. 2252), Camptothecin (Cat. No. 1100) and Mitomycin C (Cat. No. 3258)
in vitro
. Adavosertib synergizes with gemcitabine to achieve tumor regressions, selectively in p53-deficient pancreatic cancer xenografts.
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-125773 |
| Réf. fabricant | 18777586 |
| Nom chimique ou matériau | 1,2-Dihydro-1-[6-(1-hydroxy-1-methylethyl)-2-pyridinyl]-6-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-2-(2-propen-1-yl)-3 H-pyrazolo[3,4-d]pyrimidin-3-one |
| CAS | 955365-80-7 |
| Quantité | 10 mg |
| Cible | Checkpoint Control Kinase Inhibitors |
| Formule moléculaire | C<sub>27</sub>H<sub>32</sub>N<sub>8</sub>O<sub>2</sub> |
| Pureté | 98% |
