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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) CAS: 269390-77-4

Specifications
CAS Number
269390-77-4
Grade
Highly Purified
Molecular Formula
C₂₀H₁₆F₃N₃O
Molecular Weight
371.4
EU Commodity Code
38220090
Shipping Temp
Blue Ice
Storage Temp
4°C

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.
Purity
~97% (HPLC)
Concentration
Not determined
Form
Supplied as a off-white powder.
Important Note
This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
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