Luminespib
产品说明书
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同义名 : | NVP-AUY922; AUY922; VER-52296 |
| CAS号 : | 747412-49-3 | |
| 货号 : | A180168 | |
| 分子式 : | C26H31N3O5 | |
| 纯度 : | 99%+ | |
| 分子量 : | 465.54 | |
| MDL号 : | MFCD14635361 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | HSP90 (heat shock protein 90) is a cellular ubiquitous molecular chaperone responsible for promoting the conformational mutation and stabilization of several client oncoproteins, including Met, B-Raf, p53, Akt, and Kit, function of which is required by tumor cells to maintain appropriate client protein expression necessary for proliferation and survival. Luminespib is a potent HSP90 inhibitor with IC50 value of 21nM (measured by a fluorescence polarization (FP) competitive binding assay). Treatment with luminespib dose-dependently led to decreased of protein level of its client protein Her2 and Raf-1 and increased HSP72 at 16nM or 32nM for 24h and anti-proliferation with GI50 of 16nM in HCT116 cells. In vivo study showed that luminespib had a comparatively high tumor concentration with tumor/plasma ratio of 2.3 at a dose of 4mg/kg. Intraperitoneal injection of luminespib at dose of 50mg/kg, q.d., for 12 days achieved almost 50% tumor growth inhibition in HCT116 human colon carcinoma xenografts, with decreased Raf-1, Her2 and increased HSP72 at 6h after the final dose, which showed the pharmacodynamic of it[1]. | ||
| 作用机制 | Luminespib can bound to the ATP binding site of human Hsp90-alpha.[1] | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
| 22RV1 | Growth Inhibition Assay | IC50=0.03507 μM | SANGER | ||
| 23132-87 | Growth Inhibition Assay | IC50=0.10488 μM | SANGER | ||
| 5637 | Growth Inhibition Assay | IC50=0.02822 μM | SANGER | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.15mL 0.43mL 0.21mL |
10.74mL 2.15mL 1.07mL |
21.48mL 4.30mL 2.15mL |
| 参考文献 |
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