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17-AAG

替拉替尼,Tanespimycin,CP127374,CP 127374,CP-127374,NSC-330507,KOS 953,NSC330507,KOS-953,NSC 330507,KOS953

17-AAG (Tanespimycin)是一种有效的HSP90抑制剂，IC50为5 nM，作用于从肿瘤细胞提取的HSP90比作用于从正常细胞提取的HSP90结合亲和力高100倍。

目录号
EY1220
EY1220
EY1220
99.15%
纯度
99.15%
99.15%
99.15%
100 mg
规格
5 mg
10 mg
50 mg
2400
原价
390
680
1500
2400
售价
390
680
1500
现货
库存
现货
现货
EY1220
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  • 生物活性

    17-AAG is a synthetic analogue developed from geldanamycin which was found to have significant hepatic toxicity. 17-AAG has an improved toxicity profile and has no hepatic toxicity. 17-AAG can bind to HSP90 and destabilize the client proteins such as HER2, Raf-1, p53 and MAPK signaling. In Multiple myeloma (MM) cells, 17-AAG treatment inhibited cell proliferation and survival. The combination treatment of 17-AAG and bortezomib induced apoptosis in primary MM cells resistant to doxorubicin and bortezomib. The combination of 17-AAG and trastuzumab reduced the expression of ErbB2 in breast cancer cells overexpressing ErbB2. 17-AAG also showed efficacy in thyroid cancer cells and Hodgkin lymphoma cells. Besides that, 17-AAG was found to increased apoptosis in human melanoma xenografts. 17-AAG is now in phase II clinical studies.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    10 μM

  • 动物实验

    50 mg/kg 左右 腹膜注射

  • 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] Kamal A, et al. Nature, 2003, 425(6956), 407-410.
    [2] Vasilevskaya, I.A., et al. 2004. Mol. Pharmacol. 65: 235-243.
    [3] Jia, W., et al. 2003. Blood. 102: 1824-1832.
    [4] Neckers, L. 2003. Current Med. Chem. 10: 733-739.
    [5] Hostein et al (2001) Inhibition of signal transduction by the Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin results in cytostasis and apoptosis. Cancer Res. 61 4003.
    [6] Wang et al (2011) Protection of murine neural progenitor cells by the Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin in the low nanomolar concentration range. J.Neurochem. 117 703.
    [7] Schnur et al (1995) Inhibition of the oncogene product p185erbB-2 in vitro and in vivo by geldanamycin and dihydrogeldanamycin derivatives. J.Med.Chem. 38 3806.
    [8] Yang et al (2001) Disruption of the EF-2 kinase/Hsp90 protein complex: a possible mechanism to inhibit glioblastoma by geldanamycin. Cancer Res. 61 4010.

    分子式
    C31H43N3O8    		 分子量
    585.69    		 CAS号
    75747-14-7    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    ≥20 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    ≥5 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
    NCT00118248 Recurrent Thyroid Cancer|Stage IV Follicular Thyroid Cancer|Stage IV Papillary Thyroid Cancer|Thyroid Gland Medullary Carcinoma Drug: tanespimycin National Cancer Institute (NCI) Phase 2 2004-12-01 2016-12-28
    NCT00093821 Childhood Chronic Myelogenous Leukemia|Childhood Desmoplastic Small Round Cell Tumor|Disseminated Neuroblastoma|Metastatic Childhood Soft Tissue Sarcoma|Metastatic Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor|Metastatic Osteosarcoma|Previously Treated Childhood Rhabdomyosarcoma|Recurrent Childhood Acute Lymphoblastic Leukemia|Recurrent Childhood Acute Myeloid Leukemia|Recurrent Childhood Rhabdomyosarcoma|Recurrent Childhood Soft Tissue Sarcoma|Recurrent Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor|Recurrent Neuroblastoma|Recurrent Osteosarcoma Drug: tanespimycin|Other: pharmacological study|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 1 2004-09-01 2013-06-03
    NCT00087386 Recurrent Melanoma|Stage III Melanoma|Stage IV Melanoma Drug: tanespimycin|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 2 2004-06-01 2013-04-09
    NCT00096109 Recurrent Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer Drug: tanespimycin|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 2 2005-09-01 2016-11-18
    NCT00564928 Prostate Cancer|Prostatic Neoplasms|Cancer of the Prostate Drug: IPI-504 Infinity Pharmaceuticals, Inc. Phase 2 2007-11-01 2012-12-07
    NCT00113204 Multiple Myeloma Drug: IPI-504 Infinity Pharmaceuticals, Inc. Phase 1 2005-06-01 2008-05-15
    NCT00606814 Solid Tumors Drug: IPI-504, docetaxel Infinity Pharmaceuticals, Inc. Phase 1 2007-12-01 2012-03-02
    NCT00047047 Unspecified Adult Solid Tumor, Protocol Specific Drug: gemcitabine hydrochloride|Drug: tanespimycin|Drug: cisplatin|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 1 2002-08-01 2013-06-03
    NCT00779428 Advanced Malignancies Drug: Tanespimycin Bristol-Myers Squibb Phase 2 2006-07-01 2015-09-23
    NCT00969917 Dedifferentiated Liposarcoma Drug: IPI-504 Infinity Pharmaceuticals, Inc. Phase 2 2010-01-01 2015-04-13
    NCT00098488 B-cell Chronic Lymphocytic Leukemia|Prolymphocytic Leukemia|Refractory Chronic Lymphocytic Leukemia Drug: tanespimycin|Biological: rituximab National Cancer Institute (NCI) Phase 1 2005-04-01 2013-06-03
    NCT00514371 Multiple Myeloma Drug: tanespimycin|Drug: Bortezomib Bristol-Myers Squibb Phase 2|Phase 3 2007-08-01 2015-11-06
    NCT00817362 Breast Cancer|HER2 Positive Breast Cancer|Metastatic Breast Cancer|Cancer of the Breast Drug: IPI-504|Drug: Trastuzumab Infinity Pharmaceuticals, Inc. Phase 2 2009-03-01 2012-12-07
    NCT00087217 Unspecified Adult Solid Tumor, Protocol Specific Drug: tanespimycin|Drug: paclitaxel|Other: laboratory biomarker analysis|Other: pharmacological study National Cancer Institute (NCI) Phase 1 2004-05-01 2013-01-24
    NCT00773344 Solid Tumors|Breast Cancer Drug: Tanespimycin Bristol-Myers Squibb Phase 1|Phase 2 2005-12-01 2015-10-12
    NCT00079404 Acute Undifferentiated Leukemia|Recurrent Childhood Acute Lymphoblastic Leukemia|Recurrent Childhood Acute Myeloid Leukemia|Secondary Acute Myeloid Leukemia|Unspecified Childhood Solid Tumor, Protocol Specific Drug: tanespimycin National Cancer Institute (NCI) Phase 1 2004-03-01 2013-06-03
    NCT00093496 Primary Peritoneal Cavity Cancer|Recurrent Ovarian Epithelial Cancer|Stage III Ovarian Epithelial Cancer|Stage IV Ovarian Epithelial Cancer Drug: gemcitabine hydrochloride|Drug: tanespimycin National Cancer Institute (NCI) Phase 2 2007-10-01 2014-05-02
    NCT00577889 Adenocarcinoma of the Pancreas|Recurrent Pancreatic Cancer|Stage IV Pancreatic Cancer Drug: gemcitabine hydrochloride|Drug: tanespimycin National Cancer Institute (NCI) Phase 2 2008-03-01 2014-07-23

    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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