NVP-BHG712

The EphB4 receptor tyrosine kinase (cloned from erythropoietin-producing hepatocellular carcinoma) and its ligand ephrinB2 play an important role in embryonic vessel development and vascular remodeling. Signaling from this pair is also involved in tumor angiogenesis. NVP-BHG712 is an orally bioavailable inhibitor of EphB4 kinase autophosphorylation (ED50 = 25 nM). It is selective for EphB4, demonstrating an ED50 value of 4.2 µM at the related VEGFR2 receptor and ED50 values >10 µM against a panel of 40 additional kinases. At 3-30 mg/kg, NVP-BHG712 dose dependently inhibits VEGF-directed vessel formation in an in vivo mouse model of angiogenesis.Formal Name: 4-methyl-3-[[1-methyl-6-(3-pyridinyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl]amino]-N-[3-(trifluoromethyl)phenyl]-benzamide. CAS Number: 940310-85-0. Molecular Formula: C26H20F3N7O. Formula Weight: 503.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, DMSO:PBS(pH 7.2) (1:2): 0.33 mg/ml, Ethanol: 2 mg/ml. lambdamax: 257 nm. SMILES: O=C(C1=CC(NC2=C3C(N(C)N=C3)=NC(C4=CN=CC=C4)=N2)=C(C)C=C1)NC5=CC(C(F)(F)F)=CC=C5. InChi Code: InChI=1S/C26H20F3N7O/c1-15-8-9-16(25(37)32-19-7-3-6-18(12-19)26(27,28)29)11-21(15)33-23-20-14-31-36(2)24(20)35-22(34-23)17-5-4-10-30-13-17/h3-14H,1-2H3,(H,32,37)(H,33,34,35). InChi Key: ZCCPLJOKGAACRT-UHFFFAOYSA-N.