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17-AAG(KOS953)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
17-AAG(KOS953)图片
CAS NO:75747-14-7
规格:98%
分子量:585.7
包装与价格:
包装价格(元)
10mg电议
50mg电议
100mg电议
200mg电议

产品介绍
Hsp90 inhibitor
CAS:75747-14-7
分子式:C31H43N3O8
分子量:585.7
纯度:98%
存储:Store at -20°C

Background:

17-AAG is a potent inhibitor of HSP90 with IC50 value of 6 nM in BT474 cells [1].


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 [2].


参考文献:
[1] Kamal A, Thao L, Sensintaffar J, et al. A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors[J]. Nature, 2003, 425(6956): 407-410..
[2] Dimopoulos M A, Mitsiades C S, Anderson K C, et al. Tanespimycin as antitumor therapy. Clinical Lymphoma Myeloma and Leukemia, 2011, 11(1): 17-22