Potent dual specificity EGFR/HER2 inhibitor; active in vivo
Afatinib dimaleate is a potent dual specificity EGFR/HER2 inhibitor (IC50 are 0.4, 0.5, 10, 14, 1 nM for EGFRL858R, EGFRwt, EGFR L858R/T790M, ErbB2 (HER2) and ErbB4 (HER4), respectively). 100-fold more active than Gefitinib in L858R-T790M EGFR double mutant cell line. Irreversibly binds EGFR and HER2. Suppresses the kinase activity of wild-type and activated EGFR and HER2 mutants, including erlotinib-resistant isoforms. Induces tumor regression in xenograft and transgenic lung cancer models.
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-151659 |
| Réf. fabricant | 18736366 |
| Nom chimique ou matériau | (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide dimaleate |
| CAS | 850140-73-7 |
| Synonyme | BIBW2992 |
| Quantité | 50 mg |
| Formule moléculaire | C<sub>24</sub>H<sub>25</sub>ClFN<sub>5</sub>O<sub>3</sub>.2C<sub>4</sub>H<sub>4</sub>O<sub>4</sub> |
| Poids de la formule | 718.08 |
| Pureté | 98% |
