Axitinib-13C-d3 (Synonyms: AG-013736-13C-d3)

Axitinib-13C-d3 is intended for use as an internal standard for the quantification of axitinib by GC- or LC-MS. Axitinib is a VEGFR inhibitor (IC₅₀s = 1.2, 0.25, and 0.29 nM for VEGFR1, -2, and -3, respectively).¹ It also inhibits c-Kit and PDGFRβ (IC₅₀s = 1.7 and 1.6 nM, respectively). It inhibits VEGF-induced migration of and tube formation by human umbilical vein endothelial cells (HUVECs).² Axitinib (1-100 mg/kg) reduces microvessel density, a marker of angiogenesis, and tumor growth in MV522 colon carcinoma, A375 melanoma, SN12C-GFP renal carcinoma, and U87 glioma mouse xenograft models in a dose-dependent manner. Formulations containing axitinib have been used in the treatment of renal cell carcinoma.

1.Giles, F.J., Bellamy, W.T., Estrov, Z., et al.The anti-angiogenesis agent, AG-013736, has minimal activity in elderly patients with poor prognosis acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS)Leuk. Res.30(7)801-811(2006) 2.Hu-Lowe, D.D., Zou, H.Y., Grazzini, M.L., et al.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, 3Clin. Cancer Res.14(22)7272-7283(2008)