NVP-BHG712

NVP-BHG712 is a potent, orally bioavailable small molecule kinase inhibitor developed by Novartis that specifically targets the EphB4 (Ephrin type-B receptor 4) and EphA2 (Ephrin type-A receptor 2) receptor tyrosine kinases. It inhibits EphB4 kinase autophosphorylation with high potency, demonstrating IC50 values of approximately 3 nM. While it is highly selective for EphB4, it also exhibits activity against other kinases including VEGFR2, c-Raf, c-Src, and c-Abl at higher concentrations. NVP-BHG712 has been investigated in preclinical models for its anti-angiogenic and anticancer properties, demonstrating efficacy in colorectal cancer, hepatocellular carcinoma, and prostate cancer by inducing immunogenic cell death and inhibiting VEGF-driven angiogenesis. It is currently utilized as a research tool compound and is not approved for clinical use.

Other names

4-methyl-3-(1-methyl-6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamino)-N-(3-(trifluoromethyl)phenyl)benzamideCAS 940310-85-0CAS940310-85-0CAS-940310-85-0