Axitinib (AG 013736) (Synonyms: AG 013736) |
| رقم الكتالوجGC12216 |
Axitinib (AG 013736) هو مثبط متعدد الأهداف للتيروزين كيناز مع IC50s 0.1 ، 0.2 ، 0.1-0.3 ، 1.6 نانومتر لـ VEGFR1 ، VEGFR2 ، VEGFR3 و PDGFRβ ؛ ، على التوالي.
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Cas No.: 319460-85-0
Sample solution is provided at 25 µL, 10mM.
Axitinib is a selective and oral inhibitor of vascular endothelial growth factor (VEGF) receptor tyrosine kinases 1, 2 and 3 with [1].
Axitinib inhibited the phosphorylation of VEGFR-1, 2 and 3 with IC50 values of 1.2 nM, 0.2 nM and 0.1 to 0.3 nM in cells, respectively. In HUVEC cells, Axitinib inhibited VEGFR-2 stimulated cell survival with about 1000-fold selectivity against FGFR-1. Axitinib also significantly suppressed the phosphorylation of VEGF downstream signaling molecules including Akt, eNOS and ERK1/2. Besides that, axitinib inhibited VEGFR-2 phosphorylation with EC50 value of 0.49 nM in vivo. It delayed tumore growth of human xenograft tumors in mice such as M24met, HCT-116 and SN12C [1].
References:
[1] 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, 3. Clinical Cancer Research, 2008, 14(22): 7272-7283.
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