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Ganetespib
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。
Ganetespib图片
CAS NO:888216-25-9
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
STA-9090
产品介绍
Ganetespib 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。

产品描述

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

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.

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。

激酶实验

Exponentially growing cells are processed in lysis buffer (20 mM HEPES, pH 7.4, 1 mM EDTA, 5 mM MgCl2, 100 mM KCl) and incubated with increasing concentrations of 17-AAG or ganetespib for 30 min at 4°C, and incubated with biotin-GM linked to Dynabeads MyOne Streptavidin T1 magnetic beads for 1 h at 4°C. Beads are washed three times in lysis buffer and heated for 5 min at 95°C in SDS-PAGE sample buffer. Samples are resolved on 4-12% Bis-Tris gradient gel and Western blots are performed using an anti-HSP90 antibody.

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)

Cas No.

888216-25-9

分子式

C20H20N4O3

分子量

364.405

别名

STA-9090

储存和溶解度

Ethanol:<1 mgml
DMSO:38 mg/mL (104.3 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years