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Imatinib

伊马替尼,CGP057148B,ST-1571,STI571

Imatinib (STI571)是一种多靶点酪氨酸激酶抑制剂，作用于v- v-Abl， c-Kit和PDGFR 时，IC50分别为0.6， 0.1和0.1 μM。

目录号
EY0537
EY0537
EY0537
纯度
99.02%
99.02%
99.02%
规格
200 mg
500 mg
1 g
原价
420
790
1300
售价
420
790
1300
库存
现货
现货
现货
订购
订购
订购
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  • 生物活性

    The type 3 group of receptor tyrosine kinases includes PDGFR, CSF-1R, Flt-3, c-Kit and so on. PDGFRs are found in normal tissues, cells as well as some tumors. It is associated with several nonmalignant proliferative diseases. In vitro assays show that Imatinib can inhibit both PDGF-AA and PDGF-BB stimulated PDGF receptor phosphorylation. Imatinib is also found to inhibit the phosphorylation of c-Kit, another kinase which mediates the growth of a number of tumors. Imatinib inhibits the phosphorylation of these kinases without effecting the expression of them. Some other kinases of the type 3 group (such as Fms and Flt-3) can’t be inhibited by Imatinib, suggesting a selectivity of Imatinib. In addition, Imatinib is shown to significantly inhibit the Bcr-Abl tyrosine kinase both in cell-based assay and in vitro kinase assay. Moreover, as a downstream pathway of PDGF-mediated signals, MAP kinase activation can also be effected in rat A10 smooth muscle cells.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    0 - 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.

    分子式
    C29H31N7O    		 分子量
    493.6    		 CAS号
    152459-95-5    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    3 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
    NCT02177825 Plexiform Neurofibromas Drug: Imatinib Mesylate St. Justine's Hospital Phase 2 2014-06-01 2016-09-23
    NCT01140360 Neurofibromatosis|Neurofibromas Drug: Gleevec Kent Robertson|Indiana University Phase 1|Phase 2 2012-02-01 2016-08-04
    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
    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
    NCT01222013 Acute Lymphoblastic Leukemia (ALL) Philadelphia Chromosome-positive (Ph+) Drug: Imatinib Mesylate Renato Melaragno|Hospital Santa Marcelina Phase 2 null 2013-03-25
    NCT00787384 Hypereosinophilic Syndrome|Chronic Eosinophilic Leukemia|Chronic Idiopathic Hypereosinophilia Drug: Imatinib Northern Italy Leukemia Group Phase 2 2004-10-01 2010-12-28
    NCT01742299 GIST and CML Drug: STI571 Novartis Pharmaceuticals|Novartis Phase 4 2013-03-01 2016-09-09
    NCT01297777 Systemic Mastocytosis Drug: Imatinib Mesylate Hospital Virgen de la Salud Phase 4 2011-01-01 2016-08-26
    NCT00171912 Hypereosinophilic Syndrome|Systemic Mastocytosis|Chronic Myelomonocytic Leukemia|Dermatofibrosarcoma Drug: imatinib mesylate Novartis Pharmaceuticals|Novartis Phase 2 2004-09-01 2017-02-21
    NCT00424515 Mucosal Melanoma|Acral/Lentiginous Melanoma|Chronically Sun Damaged Melanomas Drug: Imatinib Dana-Farber Cancer Institute|Novartis Phase 2 2006-07-01 2016-10-16
    NCT02413736 Sarcoma Drug: Imatinib Heikki Joensuu|Scandinavian Sarcoma Group|Helsinki University Central Hospital Phase 3 2015-05-01 2016-03-04
    NCT01151852 Gastrointestinal Stromal Tumors Drug: Imatinib|Drug: Placebo Asan Medical Center Phase 3 2010-06-01 2015-06-30
    NCT00124748 Leukemia, Myeloid, Chronic Phase Drug: Imatinib mesylate Novartis Pharmaceuticals|Novartis Phase 3 2005-06-01 2012-01-05
    NCT02146846 Chronic Myelogenous Leukemia Drug: Imatinib Kerman University of Medical Sciences 2012-10-01 2016-09-02
    NCT02462538 ALK+ Anaplastic Large Cell Lymphoma Drug: Brentuximab vedotin|Drug: Imatinib Arbeitsgemeinschaft medikamentoese Tumortherapie Phase 1|Phase 2 2015-05-01 2016-05-25
    NCT01294202 Gastrointestinal Stromal Tumor (GIST) Drug: AT13387 and Imatinib Astex Pharmaceuticals Phase 2 2011-03-01 2016-01-08

    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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