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Axitinib

阿西替尼,AG 013736,AG-013736,AG013736

Axitinib是VEGFR-1， VEGFR-2，VEGFR-3，PDGFR-β和c-KIT时的多靶点抑制剂，IC50分别为0.1 nM， 0.2 nM， 0.1-0.3 nM， 1.6 nM和1.7 nM。

目录号
EY1475
EY1475
纯度
99.30%
99.30%
规格
50 mg
100 mg
原价
400
780
售价
400
780
库存
现货
现货
订购
订购
订购
订购
订购
订购
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  • 生物活性

    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.

  • 体外研究

  • 体内研究

    0.5% CMC

  • 激酶实验

  • 细胞实验

    1 nM -10 µM

  • 动物实验

    10, 30或100 mg/kg 每天口服处理

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Hu-Lowe DD, et al. Clin Cancer Res, 2008, 14(22), 7272-7283.
    [2] Wasser, K., et al.: Eur. Radiol., 13, 80 (2003)
    [3] Ma and Waxman (2008) Modulation of the antitumor activity of metronomic cyclophosphamide by the angiogenesis inhibitor axitinib. Mol.Cancer Ther. 7 79.
    [4] Pemovska et al (2015) Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation. Nature 519 102.

    分子式
    C22H18N4OS    		 分子量
    386.47    		 CAS号
    319460-85-0    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    40 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT01334112 Hepatocellular Carcinoma Drug: Axitinib (AG-013736) University Health Network, Toronto|Pfizer Phase 2 2011-01-01 2016-03-04
    NCT01562197 Glioblastoma Multiforme Drug: axitinib|Drug: Axitinib plus Lomustine Bart Neyns|Pfizer|Universitair Ziekenhuis Brussel Phase 2 2014-04-01 2016-09-08
    NCT00859118 Neoplasms Drug: AG-013736|Drug: AG-013736 University of Wisconsin, Madison|Pfizer Phase 1 2009-02-01 2015-03-04
    NCT01693822 Clear-cell Metastatic Renal Cell Carcinoma Drug: Axitinib Institute of Cancer Research, United Kingdom|Pfizer|Royal Marsden NHS Foundation Trust Phase 2 2012-10-01 2013-04-12
    NCT02700568 Carcinoma, Renal Cell|Clear Cell Renal Cell Carcinoma Drug: axitinib Kidney Cancer Research Bureau Phase 4 2016-01-01 2016-03-01
    NCT01533948 Extraocular Extension Melanoma|Metastatic Intraocular Melanoma|Recurrent Intraocular Melanoma|Recurrent Melanoma|Stage IIIA Intraocular Melanoma|Stage IIIA Melanoma|Stage IIIB Intraocular Melanoma|Stage IIIB Melanoma|Stage IIIC Intraocular Melanoma|Stage IIIC Melanoma|Stage IV Intraocular Melanoma|Stage IV Melanoma Drug: axitinib|Other: laboratory biomarker analysis Roswell Park Cancer Institute|National Cancer Institute (NCI)|National Comprehensive Cancer Network Phase 2 2012-01-01 2016-05-31
    NCT02129647 Neurofibromatosis Type 2|Vestibular Schwannomas Drug: Axitinib New York University School of Medicine Phase 2 2014-04-01 2016-10-18
    NCT02261207 Solitary Fibrous Tumor Drug: Axitinib Fondazione IRCCS Istituto Nazionale dei Tumori, Milano Phase 2 2014-11-01 2014-10-06
    NCT02164838 Refractory or Recurrent Solid Tumors, Excluding CNS Tumors Drug: Axitinib Children's Oncology Group Phase 1 2014-09-01 2017-02-13
    NCT01263769 Kidney Cancer Drug: Axitinib M.D. Anderson Cancer Center|Pfizer Phase 2 2011-02-01 2017-01-05

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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