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。
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).
1% DMSO+30% polyethylene glycol+1% Tween 80
0.001-1μM
25 mg/kg/day,持续 3 天尾部静脉注射
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。
[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
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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