RGNCY-0104 (Roxyl-ZV-5J dual CDK4/VEGFR2 inhibitor)

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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

SMILES: CC1=CC=C(NC(C2(CC2)C(NC3=CC=C(NC4=NC(C5=CC(F)=C(N=C(C)N6C(C)C

)C6=C5)=C(F)C=N4)C=C3)=O)=O)C=C1

Formula:  C33H31F2N7O2 

Mol Wt:  595.65

PMID:  31382120