Axitinib (AG 013736)

Axitinib (AG 013736)

Catalog Number:
L002369507APE
Mfr. No.:
APE-A8370
Price:
$188
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      • Overview
        • Please contact us at for specific academic pricing.

          Background

          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].

          [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.

      • Properties
        • Alternative Name
          AG 013736; N-methyl-2-[[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]sulfanyl]benzamide
          CAS Number
          319460-85-0
          Molecular Formula
          C22H18N4OS
          Molecular Weight
          386.47
          Purity
          99.01%
          Solubility
          insoluble in H2O; ≥19.3 mg/mL in DMSO; ≥3.52 mg/mL in EtOH
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Paik ES, Kim TH, et al. "Preclinical assessment of the VEGFR inhibitor axitinib as a therapeutic agent for epithelial ovarian cancer." Sci Rep. 2020;10(1):4904. > PMID:32184452
          2. Anna V. Ivanina, Ballav Borah, et al. "The Role of the Vascular Endothelial Growth Factor (VEGF) Signaling in Biomineralization of the Oyster Crassostrea gigas." Front. Mar. Sci., 28 August 2018.

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