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Axitinib

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VEGFR kinase inhibitor CAS#: 319460-85-0 Citations: 1) Hu-Lowe et al. (2008), Nonclinical antiangiogenesis and antitumor activities of axitinib (AG-013736), an oral, potent and selective inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1,2,3; Cancer Res., 14 7272 2) Ma and Waxman (2008), Modulation of the antitumor activity of metronomic cyclophosphamide by the angiogenesis inhibitor axitinib; Mol. Cancer Ther., 7 79 3) Pemovska et al. (2015), Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation; Nature, 519 102 4) Rixe et al. (2007), Axitinib treatment in patients with cytokine-refactory metastatic renal-cell cancer; a phase II study; Lancet Oncol., 8 975

Product Code: ax45112 (10 mg)

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Product Specification

Function / pharmacology Potent inhibitor of VEGFR-2, -3, and -1, IC50 = 0.2, 0.1-0.3, and 1.2 nM respectively1 displaying minimal activity against a panel of ~100 protein kinases. Inhibits angiogenesis and vascular permeability.2 Also inhibits BCR-ABL1 (T315I) with high potency, Ki = 149 pM for autophosphorylated ABL1 (T315I).3 Inhibits proliferation of Ba/F3 cells expressing BCR-ABL1 (T315I). Clinically useful anticancer agent.4
Chemical name N-Methyl-[[3-[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]benzamide
Molecular weight 386.47
Molecular formula C22H18N4OS
Physical description White solid
Solubility DMSO (30 mg/ml)
Size 10 mg
Stability Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.