Axitinib
VEGFR kinase inhibitor / 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
Biochemicals & reagents
319460-85-0
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
-20°C
TARGET: Kinase -- PATHWAY: VEGF; Proliferation -- RESEARCH AREA: Angiogenesis -- DISEASE AREA: Cancer