A cell-permeable anthranilamide that acts as a potent VEGFR inhibitor (IC50=130, 23, and 18nM against VEGFR-1, -2, and -3, respectively, IC50=1.24nM against VEGF-induced human VEGFR-2 phosphorylation in CHO cells) by targeting the ATP-binding site of VEGFR in its inactive DFG-out conformation and effectively suppresses tumor growths (50 to 100mg/kg, p.o.) via its anti-angiogenesis activity in mice and rats in vivo, while inhibiting c-kit, CSF-1R/c-Fms, PDGFR-b, and c-Abl only at higher concentrations (IC50=236, 380, 640, and 2820nM, respectively). AAL933 and two other VEGFR inhibitors, KRN633 and SU5416, are also shown to inhibit hypoxia-induced HIF-1a expression (by <90% at 30uM) and transcription activation. Unlike KRN633 and SU5416, AAL933 prevents only hypoxia-induced Erk, but not Akt, phosphorylation in HeLa cells. CAS No: 269390-77-4 Molecular Formula: C20H16F3N3O Molecular Weight: 371.4 Solubility: DMSO (100mg/ml) Storage and Stability: Lyophilized powder may be stored at -20C. Stable for 12 months at -20C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
Molecular Weight:
371.4
Purity:
~97% (HPLC)
Form:
Supplied as a off-white powder.
CAS Number:
[269390-77-4]
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