Rezivertinib (C007B-416210)

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 activityIn VitroRezivertinib (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 VivoRezivertinib (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.IC50& Target:EGFR.

Specifications and Purity: 10mM in DMSO

Molecular Formula: C27H30N6O3

Molecular Weight: 486.57