Ganetespib
作者：齐岳
发布时间：2023-08-30
09:00:47
点击数：
产品名称：Ganetespib
产品描述：
| 产品描述 | Ganetespib is a synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. |
| 靶点活性 | HSP90:4 nM |
| 体外活性 | 在多种小鼠异种移植模型中,Ganetespib表现出低毒性并且能够导致缩小.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*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) |
| 别名 | STA-9090 |
| 分子量 | 364.4 |
| 分子式 | C20H20N4O3 |
| CAS No. | 888216-25-9 |
存储
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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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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