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.1,2 It less potently inhibits c-Kit, colony stimulating factor 1 receptor, PGDF receptor β, and EGF receptor (IC50s = 236, 380, 640, and 1,040 nM, respectively) and is without effect on a number of other tyrosine kinases.1 AAL-993 is orally bioavailable in vivo, blocks VEGF-induced angiogenesis, and prevents the growth of primary tumors and spontaneous peripheral metastases in mice.1,3 It also inhibits hypoxia-mediated increase in hypoxia-inducible factor-1 transcriptional activity in an ERK-dependent manner (IC50 = ~5 µM).4WARNING This product is not for human or veterinary use.

Inhibitor of VEGFR1, 2, and 3

371.4

≥95%

Biochemicals/Kinase Inhibitors/EGFR/ErbB/HER Family/PDGFR Family/VEGFR Family/Small Molecule Inhibitors/Kinases

Formal_Name:2-[(4-pyridinylmethyl)amino]-N-[3-(trifluoromethyl)phenyl]-benzamide;Synonyms:VEGFR Tyrosine Kinase Inhibitor VI ZK 260253

O=C(NC1=CC=CC(C(F)(F)F)=C1)C2=CC=CC=C2NCC3=CC=NC=C3

C20H16F3N3O

269390-77-4

≥ 4 years

DMF: 30 mg/ml DMSO: 25 mg/ml Ethanol: 1 mg/ml

1.Manley, P.W.,Furet, P.,Bold, G., et al. Anthranilic acid amides: A novel class of antiangiogenic VEGF receptor kinase inhibitors. Journal of Medicinal Chemistry 45(26), 5687-5693 (2002).
2.Honda, T.,Tajima, H.,Kaneko, Y., et al. Conformation-activity relationship on novel 4-pyridylmethylthio derivatives with antiangiogenic activity. Bioorganic & Medicinal Chemistry Letters 18(9), 2939-2943 (2008).
3.Manley, P.W.,Bold, G.,Brüggen, J., et al. Advances in the structural biology, design and clinical development of VEGF-R kinase inhibitors for the treatment of angiogenesis. Biochim.Biophys.Acta. 1697(1-2), 17-27 (2004).
4.Ban, H.S.,Uno, M. and Nakamura, H. Suppression of hypoxia-induced HIF-1α accumulation by VEGFR inhibitors: Different profiles of AAL993 versus SU5416 and KRN633. Cancer Letters 296(1), 17-26 (2010).