BFH772

BFH772 is an inhibitor of VEGF receptor 2 (VEGFR2, IC50 = 0.0027 µM for the human receptor). It is selective for human VEGFR2 over mouse VEGFR2 and human VEGFR1 and VEGFR3 (IC50s = 1.5, 1.7, and 1.1 µM, respectively), as well as 40-fold selective over B-RAF, RET, and Tie2. BFH772 inhibits VEGF-induced proliferation of human umbilical vein endothelial cells (HUVECs, IC50 = <0.01 nM). It inhibits VEGF-induced increases in tissue weight and Tie2 levels in an angiogenesis chamber implant model in mice when administered at doses of 1 and 3 mg/kg per day. BFH772 (3 mg/kg per day) inhibits primary tumor and metastasis growth in a B16 melanoma mouse model.Formal Name: 6-[[6-(hydroxymethyl)-4-pyrimidinyl]oxy]-N-[3-(trifluoromethyl)phenyl]-1-naphthalenecarboxamide. CAS Number: 890128-81-1. Molecular Formula: C23H16F3N3O3. Formula Weight: 439.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml. lambdamax: 227 nm. SMILES: O=C(C1=CC=CC2=C1C=CC(OC3=CC(CO)=NC=N3)=C2)NC4=CC(C(F)(F)F)=CC=C4. InChi Code: InChI=1S/C23H16F3N3O3/c24-23(25,26)15-4-2-5-16(10-15)29-22(31)20-6-1-3-14-9-18(7-8-19(14)20)32-21-11-17(12-30)27-13-28-21/h1-11,13,30H,12H2,(H,29,31). InChi Key: JNLSTLQFDDAULK-UHFFFAOYSA-N.