WZ 4002 is a potent irreversible mutant selective EGFR tyrosine kinase inhibitor. It blocks ATP-dependent autophosphorylation of EGFR carrying the T790M or L858R mutation (IC50 = 8 nM). WZ 4002 exhibits selectivity for mutant EGFR over wild-type. In mice bearing T790M mutant lung cancer cell lines WZ 4002 inhibits EGFR, AKT and ERK1/2 phosphorylation and results in significant tumor regression.
Caractéristiques techniques
| Marque | Tocris Bioscience |
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| Réf. B-LABO | BL-RE-125581 |
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| Réf. fabricant | 18718636 |
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| Nom chimique ou matériau | N-[3-[[5-Chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-2-propenamide |
|---|
| CAS | 1213269-23-8 |
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| Quantité | 10 mg |
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| Cible | EGF Receptor Inhibitors |
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| Formule moléculaire | C<sub>25</sub>H<sub>27</sub>ClN<sub>6</sub>O<sub>3</sub> |
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| Pureté | 0.98 |
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