AAL-993 is a highly potent inhibitor of Flt-1 (VEGFR-1), Flk-1 (VEGFR-2) and Flt-4 (VEGFR-3) (IC50=130nM, IC50=23nM and IC50=18nM respectively). At higher concentrations it inhibits PDGFR-β (640nM), c-Kit (236nM) and c-Fms-CSF-1R (CSF-1R) (380nM). AAL-993 shows no activity towards other kinases such as EGFR, FGFR-1, CDK-1, Tie-2, c-Met, IGF-1R, c-Src and c-Abl. An X-ray crystal structure of AAL-993 complexed with the catalytic domain of diphosphorylated VEGFR-2 indicates that this molecule binds to an inactive conformation of the protein.
Soluble in ethanol (15 mg/ml), and DMSO (>25 mg/ml).
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