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VEGFR Tyrosine Kinase Inhibitor VI, AAL-993
2-((4-Pyridyl)methyl)amino-N-(3-(trifluoromethyl)phenyl)benzamide, ZK260253, VEGFR2 Kinase Inhibitor XXXIII, VEGFR1 Kinase Inhibitor VIII, VEGFR3 Kinase Inhibitor VII, AAL993, PDGFR Tyrosine Kinase Inhibitor XXIII
A cell-permeable anthranilamide that acts as a potent VEGFR inhibitor (IC50 = 130, 23, and 18 nM against VEGFR-1, -2, and -3, respectively; IC50 = 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 (IC50 = 236, 380, 640, and 2820 nM, respectively). AAL933 and two other VEGFR inhibitors, KRN633 and SU5416 (Cat. No. 676487), are also shown to inhibit hypoxia-induced HIF-1α expression (by <90% at 30 µM) and transcription activation. Unlike KRN633 and SU5416, AAL933 prevents only hypoxia-induced Erk, but not Akt, phosphorylation in HeLa cells.
产品信息
Form Off-white powder
Molar mass 371.4
Protect from Light 是的
Packaged under inert gas 是的
Purity ≥97% by HPLC
Solubility DMSO
Chemical formula C20H16F3N3O
CAS number 269390-77-4
商店和运输信息
Storage +2°C to +8°C
Ship Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Regulatory Review |