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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Heat Shock Protein (HSP)-Gamitrinib TPP hexafluorophosphate
Gamitrinib TPP hexafluorophosphate

Chemical Structure : Gamitrinib TPP hexafluorophosphate

CAS No.: 1131626-47-5

Gamitrinib TPP hexafluorophosphate

货号: PC-38121Not For Human Use, Lab Use Only.

Gamitrinib is a small molecule mitochondrial Hsp90 inhibitor, selectively targets Hsp90 network in tumor mitochondria.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Gamitrinib is a small molecule mitochondrial Hsp90 inhibitor, selectively targets Hsp90 network in tumor mitochondria.
Gamitrinibs were shown to accumulate in the mitochondria of human tumor cell lines and to inhibit Hsp90 activity by acting as ATPase antagonists.
Unlike Hsp90 antagonists not targeted to mitochondria, Gamitrinibs exhibited a "mitochondriotoxic" mechanism of action, causing rapid tumor cell death and inhibiting the growth of xenografted human tumor cell lines in mice.
Gamitrinib is not toxic to normal cells or tissues and did not affect Hsp90 homeostasis in cellular compartments other than mitochondria.

物理化学性质&存储条件

分子量 1036.04
分子式 C52H65F6N3O8P2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(6-(((4E,6Z,8S,9S,10E,12S,13R,14S,16R)-9-(carbamoyloxy)-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-19-yl)amino)hexyl)triphenylphosphonium hexafluorophosphate(V)

参考文献

1. Wei S, et al. Clin Cancer Res. 2022 Mar 4:clincanres.0833.2021.

2. Kang BH, et al. J Clin Invest. 2009 Mar;119(3):454-64.

3. Kang BH, et al. Br J Cancer. 2011 Feb 15;104(4):629-34.

4. Park HK, et al. Mol Cancer. 2014 Jun 12;13:148.

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