ABT-869

ABT-869 is a dual VEGFR and PDGFR family kinase inhibitor (IC50s = 0.003, 0.004, 0.004, 0.19, 0.066, 0.003, and 0.014 µM for VEGFR1, VEGFR2, FLT3, VEGFR3, PDGFRbeta, CSF-1R, and KIT, respectively). It is selective for these kinases over other tyrosine kinases, including RET, FGFR, Src, EGFR, and c-Met (IC50s = 1.9, >12.5, >50, >50, and >50 µM, respectively), but also inhibits Tie2 (IC50 = 0.17 µM). ABT-869 inhibits the proliferation of HT-29 colon and MDA-MB-435 breast cancer, 9L glioma, and MV4-11 acute myeloid leukemia cells (IC50s = 1.3, 2.4, 0.27, and 0.004 µM, respectively). It induces apoptosis in MV4-11 cells (IC50 = 0.03 µM) and inhibits VEGF-induced uterine edema in mice (ED50 = 0.5 mg/kg). ABT-869 (1, 3, and 10 mg/kg) improves survival in a MOLM-13 leukemia mouse xenograft model.Formal Name: N-[4-(3-amino-1H-indazol-4-yl)phenyl]-N'-(2-fluoro-5-methylphenyl)-urea. CAS Number: 796967-16-3. Synonyms: Linifanib. Molecular Formula: C21H18FN5O. Formula Weight: 375.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 25 mg/ml, DMSO:PBS (pH 7.2) (1:5): 0.2 mg/ml. lambdamax: 271, 323 nm. SMILES: NC1=NNC2=C1C(C3=CC=C(NC(NC4=C(F)C=CC(C)=C4)=O)C=C3)=CC=C2. InChi Code: InChI=1S/C21H18FN5O/c1-12-5-10-16(22)18(11-12)25-21(28)24-14-8-6-13(7-9-14)15-3-2-4-17-19(15)20(23)27-26-17/h2-11H,1H3,(H3,23,26,27)(H2,24,25,28). InChi Key: MPVGZUGXCQEXTM-UHFFFAOYSA-N.