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Ganetespib

STA-9090

Ganetespib (STA-9090)是一种HSP90抑制剂,作用于OSA 8种细胞,IC50为4 nM,诱导OSA细胞凋亡,而对正常的成骨细胞无作用;是STA-1474的活性代谢物。

目录号
EY1224
EY1224
EY1224
纯度
99.42%
99.42%
99.42%
规格
1 mg
5 mg
10 mg
原价
280
680
880
售价
280
680
880
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Ganetespib (STA-9090) is a potent synthetic small molecule inhibitor of Hsp90 with potential antineoplastic activity. Ganetespib has an IC50 value 10–50 times lower than that for 17-AAG against malignant mast cell lines, indicating that the triazolone class of HSP90 inhibitors is likely more potent than geldanamycin based inhibitors. Ganetespib inhibits MG63 cell lines (IC50 of 43 nM).

  • 体外研究

  • 体内研究

    1% DMSO+30% polyethylene glycol+1% Tween 80

  • 激酶实验

  • 细胞实验

    0.001-1μM

  • 动物实验

    25 mg/kg/day,持续 3 天尾部静脉注射

  • 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 AKm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] McCleese Jk, et al. Int J Cancer. 2009, 125(12), 2792-2801.

    分子式
    C20H20N4O3
    分子量
    364.4
    CAS号
    888216-25-9
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    ≥70 mg/mL
    Water
    <1 mg/mL
    Ethanol
    ≥15 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
    NCT01554969 Rectal Cancer Drug: capecitabine + ganetespib Emory University|Synta Pharmaceuticals Corp. Phase 1 2012-05-01 2016-02-19
    NCT01485835 Multiple Myeloma Drug: Ganetespib|Drug: Bortezomib|Drug: Dexamethasone Emory University|Multiple Myeloma Research Consortium|Synta Pharmaceuticals Corp. Phase 1 2012-01-01 2015-10-08
    NCT02008877 Malignant Peripheral Nerve Sheath Tumors (MPNST)|Sarcoma Drug: ganetespib|Drug: Sirolimus Sarcoma Alliance for Research through Collaboration|Synta Pharmaceuticals Corp.|United States Department of Defense Phase 1|Phase 2 2013-12-01 2016-10-12
    NCT01560416 Breast Cancer Drug: Fulvestrant|Drug: Ganetespib Dana-Farber Cancer Institute Phase 2 2012-05-01 2017-01-17
    NCT01562015 Non Small Cell Lung Cancer Drug: Ganetespib Synta Pharmaceuticals Corp. Phase 2 2012-04-01 2015-05-18
    NCT02261805 Cancer|Small Cell Lung Cancer Drug: Ganetespib and doxorubicin Georgetown University|Synta Pharmaceuticals Corp. Phase 1|Phase 2 2014-10-01 2016-12-30
    NCT01798485 Non-Small-Cell Lung Adenocarcinoma|Non-small Cell Lung Cancer Stage IIIB|Non-small Cell Lung Cancer Stage IV|Non-small Cell Lung Cancer Metastatic Drug: Docetaxel|Drug: Ganetespib Synta Pharmaceuticals Corp. Phase 3 2013-04-01 2016-05-26
    NCT01039519 Gastrointestinal Stromal Tumor Drug: Ganetespib Synta Pharmaceuticals Corp. Phase 2 2010-01-01 2016-02-11
    NCT01579994 Advanced Lung Cancer Drug: Ganetespib (STA-9090) and crizotinib Memorial Sloan Kettering Cancer Center Phase 1 2012-04-01 2017-03-13
    NCT00687934 Solid Tumors Drug: STA-9090 Synta Pharmaceuticals Corp. Phase 1 2007-10-01 2014-09-17
    NCT01962948 Recurrent Fallopian Tube Cancer|Recurrent Ovarian Epithelial Cancer|Recurrent Primary Peritoneal Cavity Cancer Drug: paclitaxel|Drug: ganetespib|Other: laboratory biomarker analysis Fox Chase Cancer Center|National Cancer Institute (NCI) Phase 1|Phase 2 2013-10-01 2016-11-23
    NCT02389751 Esophageal Cancer Drug: Ganetespib|Drug: Carboplatin|Drug: Paclitaxel|Radiation: Radiotherapy M.D. Anderson Cancer Center|Synta Pharmaceuticals Corp. Phase 1 2015-04-01 2017-03-13
    NCT02060253 HER2-positive Breast Cancer|Male Breast Cancer|Recurrent Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer Drug: ganetespib|Drug: paclitaxel|Biological: trastuzumab|Biological: pertuzumab Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI)|Synta Pharmaceuticals Corp.|New York University Cancer Institute Phase 1 2014-04-01 2016-07-11
    NCT01183364 Solid Tumor Malignancies Drug: STA-9090 (ganetespib) with Docetaxel Synta Pharmaceuticals Corp. Phase 1 2010-07-01 2014-09-18
    NCT00688116 Solid Tumors Drug: STA 9090 (ganetespib) Synta Pharmaceuticals Corp. Phase 1 2007-10-01 2014-09-17
    NCT01677455 Breast Cancer|HER-2 Positive Breast Cancer|Triple Negative Breast Cancer|ER/Progressive Response (PR) + Refractory to Prior Hormonal Treatment Drug: ganetespib Synta Pharmaceuticals Corp. Phase 2 2012-07-01 2015-11-04
    NCT01167114 Esophagogastric Cancer Drug: STA-9090 Massachusetts General Hospital|Dana-Farber Cancer Institute|Beth Israel Deaconess Medical Center|Synta Pharmaceuticals Corp. Phase 2 2010-08-01 2017-01-06
    NCT01665937 Hepatocellular Carcinoma Drug: STA-9090 Massachusetts General Hospital|Dana-Farber Cancer Institute|Beth Israel Deaconess Medical Center|Synta Pharmaceuticals Corp. Phase 1 2010-08-01 2014-03-19
    NCT01590160 Lung Cancer - Malignant Pleural Mesothelioma Drug: Ganetespib University College, London|Cancer Research UK Phase 1|Phase 2 2013-08-01 2016-10-26
    NCT01368003 Adenocarcinoma of the Prostate Drug: STA9090|Drug: STA9090 with Dutasteride Toni Choueiri, MD|Dana-Farber Cancer Institute Phase 2 2011-04-01 2015-08-29
    NCT02012192 Epithelial Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Cancer Drug: Ganetespib|Drug: Paclitaxel Medical University Innsbruck|European Commission Phase 1|Phase 2 2014-06-01 2016-12-05

    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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