Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 253 | 现货 | ||
5 mg | ¥ 573 | 现货 | ||
10 mg | ¥ 828 | 现货 | ||
25 mg | ¥ 1,260 | 现货 | ||
50 mg | ¥ 1,580 | 现货 | ||
100 mg | ¥ 2,320 | 现货 | ||
200 mg | ¥ 3,450 | 现货 | ||
500 mg | ¥ 5,590 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 653 | 现货 |
产品描述 | Ganetespib (STA-9090) 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) |
别名 | STA-9090 |
分子量 | 364.4 |
分子式 | C20H20N4O3 |
CAS No. | 888216-25-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 38 mg/mL (104.3 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.7442 mL | 13.7212 mL | 27.4424 mL | 68.6059 mL |
5 mM | 0.5488 mL | 2.7442 mL | 5.4885 mL | 13.7212 mL | |
10 mM | 0.2744 mL | 1.3721 mL | 2.7442 mL | 6.8606 mL | |
20 mM | 0.1372 mL | 0.6861 mL | 1.3721 mL | 3.4303 mL | |
50 mM | 0.0549 mL | 0.2744 mL | 0.5488 mL | 1.3721 mL | |
100 mM | 0.0274 mL | 0.1372 mL | 0.2744 mL | 0.6861 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Ganetespib 888216-25-9 Angiogenesis Apoptosis Chromatin/Epigenetic Cytoskeletal Signaling Metabolism HSP HIF Heat shock proteins inhibit Inhibitor STA 9090 STA9090 STA-9090 inhibitor