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Ganetespib

Ganetespib (STA-9090) 是一种热休克蛋白 90 抑制剂，通过抑制 HIF-1α 和 STAT3 对大肠癌具有抗血管生成作用。它还具有细胞毒性。

CAS号

888216-25-9

分子式

C20H20N4O3

主要靶点

HSP|HIF|Apoptosis

仅限科研使用

Cat No : CM04644

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Synonyms

STA-9090

验证数据展示

  • CAS No.: 888216-25-9

    Ganetespib
    CAS#: 888216-25-9

产品信息

Ganetespib is a synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity.

CAS号 888216-25-9
分子式 C20H20N4O3
主要靶点 HSP|HIF|Apoptosis
主要通路 血管生成|代谢|凋亡|细胞骨架|表观遗传
分子量 364.4
纯度 97.29%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 STA-9090

靶点活性

HSP90:4 nM

体内活性

在多种人类抗受体酪氨酸激酶抑制剂和抗塔培霉素的癌细胞系中,Ganetespib在纳摩尔级别能够表现出细胞毒性,抑制细胞增殖,同时诱导细胞凋亡。在MG63细胞系中（IC50=43 nM）,Ganetespib抑制细胞生长。在C2（IC50=19 nM）和BR犬恶性肥大细胞（IC50=4 nM）中,Ganetespib诱导细胞凋亡。

体外活性

在多种小鼠肿瘤异种移植模型中,Ganetespib表现出低毒性并且能够导致肿瘤缩小.其中,在恶性肥大细胞和OSA异种移植物模型中,Ganetespib（25 mg / kg /day）具有良好的安全性,并且能够抑制肿瘤细胞的生长.

溶解度

Ethanol:<1 mg/mL,DMSO:38 mg/mL (104.3 mM),H2O:<1 mg/mL

细胞实验

A total of 1.5 × 103 OSA cells are seeded in 96-well plates in 10% serum-containing complete medium and incubated overnight to determine the 50% inhibitory concentrations. Plates are, harvested at day 5 following 0.001, 0.005, 0.01, 0.05, 0.1, 0.5 and 1 μM Ganetespib, treatment and analyzed. Fluorescence measurements are made using a plate reader with excitation at 485 nm and emission detection at 530 nm. Relative cell number is calculated as a percentage of the control wells: absorbance of sample/absorbance of DMSO treated cells × 100.(Only for Reference)

参考文献

1.McCleese Jk, et al. Int J Cancer. 2009, 125(12), 2792-2801.
2.Wang Y, et al. Curr Opin Investig Drugs. 2010 , 11(12), 1466-1476.
3.Ying W, et al. Mol Cancer Ther. 2012, 11(2), 475-484.
4.Lin TY, et al. Exp Hematol. 2008, 36(10), 1266-1277.
5.Peng Y C, Wang S, Zhang Y, et al. Hsp90β inhibitors prevent GLT-1 degradation but have no beneficial efficacy on absence epilepsy[J]. Journal of Asian natural products research. 2018 Nov 17:1-11.

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