Roxyl-ZV-5J dual CDK4/VEGFR2 inhibitor RGNCY-0104
Per 10 mg
Roxyl-ZV-5J is a potent dual inhibitor of CDK4 and VEGFR2 (IC50 of 46nM for each). Roxyl-ZV-5J significantly induced breast and cervical cancer cell cycle arrest and cell apoptosis. In HUVEC cells, Roxyl-ZV-5J also inhibited the the proliferation, tube formation and VEGFR2 downstream signalling pathways. The oral administration of Roxyl-ZV-5J resulted insignificant tumor regression and anti-angiogenesis in the SiHa xenograft mouse model without apparent toxicity. Roxyl-ZV-5J also exhibited a good pharmacokinetic profile.
Systematic Name: N-(4-((5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazol-6-yl)pyrimidin-2-yl)amino)phenyl)-N-(p-tolyl)cyclopropane-1,1-dicarboxamide
Mol Wt: 595.65
Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. Huang Z et al. Eur J Med Chem. 2019 Jul 28;181:111541.
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