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217866

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)

Size

£386.00

SKU:
217866
Molecular Weight:
371.4
Purity:
~97% (HPLC)
Storage Conditions:
4°C
Supplier:
United States Biological
CAS Number:
269390-77-4
Format:
Supplied as a off-white powder.
Extra Details:
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 -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. 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.
Shipping Conditions:
Blue Ice