AAL-993

• CAT Number: R062353
• CAS Number: 269390-77-4
• Molecular Formula: C20H16F3N3O
• Molecular Weight: 371.363
• Purity: ≥95%
• Synonyms: ZK260253; 2-​​[(4-​​Pyridinylmethyl)​amino]​-​​N-​​[3-​​(trifluoromethyl)​phenyl]​benzamide; 2-((Pyridin-4-ylmethyl)amino)-N-(3-(trifluoromethyl)phenyl)benzamide
• Target: VEGFR
• Solubility: Soluble in DMSO
• Storage: Store at -20°C
• IUPAC Name: 2-(pyridin-4-ylmethylamino)-N-[3-(trifluoromethyl)phenyl]benzamide
• InChI: 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)
• InChIKey: BLAFVGLBBOPRLP-UHFFFAOYSA-N
• SMILES: C1=CC=C(C(=C1)C(=O)NC2=CC=CC(=C2)C(F)(F)F)NCC3=CC=NC=C3

AAL-993 is a highly potent inhibitor of VEGFR-1 (IC50 =130nM), VEGFR-2 (IC50=23nM) and VEGFR-3 (IC50=18nM). At higher concentrations it inhibits PDGFR-β (640nM), c-Kit (236nM) and CSF-1R (380nM).

Reference

1: Ban HS, Uno M, Nakamura H. Suppression of hypoxia-induced HIF-1alpha accumulation by VEGFR inhibitors: Different profiles of AAL993 versus SU5416 and KRN633. Cancer Lett. 2010 Oct 1;296(1):17-26. doi: 10.1016/j.canlet.2010.03.010. Epub 2010 Apr 7. PubMed PMID: 20378243.2: Honda T, Tajima H, Kaneko Y, Ban M, Inaba T, Takeno Y, Okamoto K, Aono H. Conformation-activity relationship on novel 4-pyridylmethylthio derivatives with antiangiogenic activity. Bioorg Med Chem Lett. 2008 May 1;18(9):2939-43. doi: 10.1016/j.bmcl.2008.03.068. Epub 2008 Mar 29. PubMed PMID: 18420406.3: Manley PW, Bold G, Brüggen J, Fendrich G, Furet P, Mestan J, Schnell C, Stolz B, Meyer T, Meyhack B, Stark W, Strauss A, Wood J. Advances in the structural biology, design and clinical development of VEGF-R kinase inhibitors for the treatment of angiogenesis. Biochim Biophys Acta. 2004 Mar 11;1697(1-2):17-27. Review. PubMed PMID: 15023347.