Ganetespib
作者：齊岳
發(fā)布時間：2023-08-30
09:00:47
點擊數(shù)：
產(chǎn)品名稱：Ganetespib
產(chǎn)品描述：
| 產(chǎn)品描述 | Ganetespib is a synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. |
| 靶點活性 | HSP90:4 nM |
| 體外活性 | 在多種小鼠腫瘤異種移植模型中,Ganetespib表現(xiàn)出低毒性并且能夠?qū)е履[瘤縮小.其中,在惡性肥大細(xì)胞和OSA異種移植物模型中,Ganetespib（25 mg / kg /day）具有良好的安全性,并且能夠抑制腫瘤細(xì)胞的生長. |
| 體內(nèi)活性 | 在多種人類抗受體酪氨酸激酶抑制劑和抗塔培霉素的癌細(xì)胞系中,Ganetespib在納摩爾級別能夠表現(xiàn)出細(xì)胞毒性,抑制細(xì)胞增殖,同時誘導(dǎo)細(xì)胞凋亡。在MG63細(xì)胞系中（IC50=43 nM）,Ganetespib抑制細(xì)胞生長。在C2（IC50=19 nM）和BR犬惡性肥大細(xì)胞（IC50=4 nM）中,Ganetespib誘導(dǎo)細(xì)胞凋亡。 |
| 激酶實驗 | 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. |
| 細(xì)胞實驗 | 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) |
| 別名 | STA-9090 |
| 分子量 | 364.4 |
| 分子式 | C20H20N4O3 |
| CAS No. | 888216-25-9 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
Ethanol: <1 mg/mL
DMSO: 38 mg/mL (104.3 mM)
H2O: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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