AAL-993 Chemische Eigenschaften,Einsatz,Produktion Methoden
Allgemeine Beschreibung
A cell-permeable anthranilamide that acts as a potent VEGFR inhibitor (IC
50 = 130, 23, and 18 nM against VEGFR-1, -2, and -3, respectively; IC
50 = 1.24 nM 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 100 mg/kg; p.o.) via its anti-angiogenesis activity in mice and rats
in vivo, while inhibiting c-kit, CSF-1R/c-Fms, PDGFR-β, and c-Abl only at higher concentrations (IC
50 = 236, 380, 640, and 2820 nM, respectively). AAL933 and two other VEGFR inhibitors, KRN633 and SU5416, are also shown to inhibit hypoxia-induced HIF-1α expression (by <90% at 30 M) and transcription activation. Unlike KRN633 and SU5416, AAL933 prevents only hypoxia-induced Erk, but not Akt, phosphorylation in HeLa cells.
AAL-993 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
