RGNCY-0072 (R916562 Axl/VEGF-R2 inhibitor)

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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.

SMILE:  [H][C@]1(C2)[C@H](C[C@]2([H])CC1)N3CCN(C4=CC=C(NC5=NN(C6=NC(Cl)

=NC7=C6SC=C7C)C(N)=N5)C=C4)CC3

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

Formula:  C26H30ClN9S

PMID:  28711351