RGNCY-0072 (R916562 Axl/VEGF-R2 inhibitor)
R916562 is a potent dual inhibitor of Axl and VEGF-R2. R916562 is suitable for oral delivery and and shows activity comparable to the clinically approved tyrosine kinase inhibitor Sunitinib in mouse xenograft models (MDA-MB-321human breast cancer cells and CaKi-1 human renal carcinoma) and the corneal micropocket angiogenesis model. The inhibition of both Axl and VEGF-R2 may be more effective in preventing angiogenesis and tumor growth than targeting either receptor alone and may be of benefit for patients relapsing after VEGF-R2 targeted therapy.
Systematic Name: N3-(4-(4-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-yl)piperazin-1-yl)phenyl)-1-(2-chloro-7-methylthieno[3,2-d]pyrimidin-4-yl)-1H-1,2,4-triazole-3,5-diamine
Molecular Weight: 536.10
Tags: Cancer, breast cancer, Tumor, RGNCY-0072, R916562, Axl, VEGF-R2, angiogenesis, renal carcinoma