Home > Bcr-Abl & c-Kit & PDGFR & > Imatinib Mesylate

Imatinib Mesylate

甲磺酸伊马替尼,STI571,CGP-57148B,ST-1571 Mesylate

Imatinib Mesylate (STI571)是Imatinib的甲磺酸盐，具有较好的口服生物利用度，是一种多靶点的抑制剂，同时作用于v-Abl， c-Kit和PDGFR，IC50分别为0.6 μM， 0.1 μM 和0.1 μM。

目录号
EY0363
EY0363
EY0363
纯度
99.13%
99.13%
99.13%
规格
100 mg
200 mg
500 mg
原价
220
450
840
售价
220
450
840
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
具体折扣请咨询客服

  • 生物活性

    Imatinib Mesylate is a specific tyrosine kinase (abl, c-kit, and PDGFR) inhibitor and is reported to sensitize cells to radio- or chemo-therapy. When tested with Y-79 and WERI-RB-1 Rb cell lines, imatinib mesylate treatment decreased the cell proliferation and invasion with the concentration of 10 μM . In osteoblast cells, administration of imatinib mesylate decreased osteoclast development via stimulating differentiation, inhibiting proliferation and survival.

  • 体外研究

  • 体内研究

    Saline

  • 激酶实验

  • 细胞实验

    100 μM

  • 动物实验

    70或100 mg/kg 腹腔注射

  • 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] Buchdunger E, et al. Proc Natl Acad Sci USA, 1995, 92(7), 2558–2562.
    [2] Buchdunger, E., et al. 2000. J. Pharmacol. Exp. Ther. 295: 139-145.
    [3] Boucher, P., et al. 2003. Science. 300: 329-332.

    分子式
    C29H31N7O.CH4SO3    		 分子量
    589.7    		 CAS号
    220127-57-1    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    200 mg/mL    		 Water
    200 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
    NCT01140360 Neurofibromatosis|Neurofibromas Drug: Gleevec Kent Robertson|Indiana University Phase 1|Phase 2 2012-02-01 2016-08-04
    NCT00702689 Sclerotic Graft Versus Host Disease|Imatinib Mesylate Drug: Gleevec, STI571(Imatinib Mesylate) National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Phase 2 2008-05-01 2015-09-29
    NCT02177825 Plexiform Neurofibromas Drug: Imatinib Mesylate St. Justine's Hospital Phase 2 2014-06-01 2016-09-23
    NCT00171912 Hypereosinophilic Syndrome|Systemic Mastocytosis|Chronic Myelomonocytic Leukemia|Dermatofibrosarcoma Drug: imatinib mesylate Novartis Pharmaceuticals|Novartis Phase 2 2004-09-01 2017-02-21
    NCT01297777 Systemic Mastocytosis Drug: Imatinib Mesylate Hospital Virgen de la Salud Phase 4 2011-01-01 2016-08-26
    NCT01221376 Chronic Myeloid Leukemia (CML) With Philadelphia Chromosome-positive (Ph+) Drug: Imatinib Mesylate Renato Melaragno|Hospital Santa Marcelina Phase 2 2011-02-01 2013-03-25
    NCT01222013 Acute Lymphoblastic Leukemia (ALL) Philadelphia Chromosome-positive (Ph+) Drug: Imatinib Mesylate Renato Melaragno|Hospital Santa Marcelina Phase 2 null 2013-03-25
    NCT00090987 Sarcoma Drug: imatinib mesylate AIDS Malignancy Consortium|National Cancer Institute (NCI)|The EMMES Corporation Phase 2 2005-06-01 2014-08-27
    NCT00038675 Chronic Myelomonocytic Leukemia|Chronic Myeloid Leukemia|Polycythemia Vera|Hypereosinophilic Syndrome|Mastocytosis Drug: Imatinib Mesylate (Gleevec) M.D. Anderson Cancer Center|Novartis Pharmaceuticals 2001-06-01 2013-12-10
    NCT00613054 Glioblastoma|Gliosarcoma Drug: Zactima, Gleevec, Hydroxyurea Annick Desjardins|Novartis Pharmaceuticals|AstraZeneca|Duke University Phase 1 2007-11-01 2012-12-04
    NCT00080665 Breast Cancer Drug: docetaxel|Drug: imatinib mesylate Sidney Kimmel Comprehensive Cancer Center|National Cancer Institute (NCI) Phase 1 2003-12-01 2016-11-04
    NCT02303899 Mesothelioma, Malignant Drug: Gemcitabine|Drug: Imatinib mesylate Istituto Clinico Humanitas Phase 2 2014-11-01 2017-02-09
    NCT00136409 Myelofibrosis|Myeloid Metaplasia|Agnogenic Myeloid Metaplasia|Chronic Myelomonocytic Leukemia Drug: Imatinib mesylate Dana-Farber Cancer Institute|Brigham and Women's Hospital|Massachusetts General Hospital|Novartis Phase 2 2002-05-01 2016-12-22
    NCT00237185 Unresectable or Metastatic Malignant Gastrointestinal Stromal Tumor (GIST) Drug: Imatinib mesylate Novartis Pharmaceuticals|Novartis Phase 2 2000-06-01 2014-08-14
    NCT00354913 Glioblastoma|Gliosarcoma Drug: hydroxyurea|Drug: imatinib mesylate Duke University|National Cancer Institute (NCI)|Novartis Pharmaceuticals Phase 2 2005-05-01 2013-01-14
    NCT00154349 Philadelphia Chromosome Positive Acute Lymphocytic Leukemia Drug: Imatinib Mesylate Novartis Pharmaceuticals|Novartis Phase 2 2003-10-01 2017-02-21
    NCT01742299 GIST and CML Drug: STI571 Novartis Pharmaceuticals|Novartis Phase 4 2013-03-01 2016-09-09
    NCT00787384 Hypereosinophilic Syndrome|Chronic Eosinophilic Leukemia|Chronic Idiopathic Hypereosinophilia Drug: Imatinib Northern Italy Leukemia Group Phase 2 2004-10-01 2010-12-28

    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。

  • 相关化合物库

  • 使用AMQUAR产品发表文献后请联系我们

相关推荐

X
  • 联系人 ：
  • 收件地址 ：
  • 电话号码 ：
  • 单位名称 ：
  • 产品货号 ：
  • 产品规格 ：
  • 发票抬头以及单位税号 ：