AAL-993

AAL-993 is a potent inhibitor of VEGF receptors, inhibiting VEGFR1, 2, and 3 with IC50 values of 130, 23, and 18 nM, respectively. It less potently inhibits c-Kit, colony stimulating factor 1 receptor, PGDF receptor beta, and EGF receptor (IC50s = 236, 380, 640, and 1,040 nM, respectively) and is without effect on a number of other tyrosine kinases. AAL-993 is orally bioavailable in vivo, blocks VEGF-induced angiogenesis, and prevents the growth of primary tumors and spontaneous peripheral metastases in mice. It also inhibits hypoxia-mediated increase in hypoxia-inducible factor-1 transcriptional activity in an ERK-dependent manner (IC50 = ~5 µM).Formal Name: 2-[(4-pyridinylmethyl)amino]-N-[3-(trifluoromethyl)phenyl]-benzamide. CAS Number: 269390-77-4. Synonyms: VEGFR Tyrosine Kinase Inhibitor VI, ZK 260253. Molecular Formula: C20H16F3N3O. Formula Weight: 371.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 25 mg/ml, Ethanol: 1 mg/ml. lambdamax: 220, 256, 348 nm. SMILES: O=C(NC1=CC=CC(C(F)(F)F)=C1)C2=CC=CC=C2NCC3=CC=NC=C3. InChi Code: InChI=1S/C20H16F3N3O/c21-20(22,23)15-4-3-5-16(12-15)26-19(27)17-6-1-2-7-18(17)25-13-14-8-10-24-11-9-14/h1-12,25H,13H2,(H,26,27). InChi Key: BLAFVGLBBOPRLP-UHFFFAOYSA-N.