Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity In Vitro Rezivertinib (BPI-7711) selectively inhibits cellular proliferation of EGFR mutations in cell lines: GI 50 13.3 nM (PC9, del19), 6.8 nM (HCC827, L858R), 22 nM (NCI-H1975, del19/T790M) and > 1000 nM (A431, EGFR WT). MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Rezivertinib (BPI-7711; 6.25-25 mg/kg/day; orally; 14 days) shows significant tumor regression. Rezivertinib (12.5 mg/kg/day; orally; 14 days) survives an average of 112% longer in H1975-luc human NSCLC mice model. Rezivertinib (50 mg/kg/day; orally) has anti-tumor efficacy correlated to improved average overall survival of the animals of 115% (28 days vs. 13 days). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:EGFR
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Rezivertinib
CAS number：1835667-12-3 molecular formula：C27H30N6O3
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| Chinese alias | 瑞替尼 | ||
| English alias | 2-Propenamide, N-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl)amino)phenyl)- | N-(2-(2-(Dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl)amino)phenyl)-2-propenamide | HY-109189 | 2-Propena | ||
| CAS number | 1835667-12-3 | molecular formula | C27H30N6O3 |
| molecular weight | 486.57 g/mol | Exact mass | ≥99% |
| PSA | 93.500 Ų | logp | 3.600 |
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