Name | Luminespib |
Description | Luminespib (VER-52296) is an HSP90 inhibitor that inhibits HSP90α and HSP90β (IC50=7.8/21 nM). Luminespib has antitumor activity and is used in studies of head and neck tumors, among others. |
Cell Research | Cell lines were grown in DMEM/10% FCS, 2 mmol/L glutamine, and nonessential amino acids in a humidified atmosphere of 5% CO2 in air. All lines were free of Mycoplasma. Cell proliferation was determined using the sulforhodamine B (SRB) assay for tumor cells and prostate epithelial cells, the WST-1 assay for MCF10A and HB119, or an alkaline phosphatase assay for HUVEC and HDMEC. GI50 was the compound concentration inhibiting cell proliferation by 50% compared with vehicle controls. Cell cycle analysis was as described. Active caspase-3/7 was measured using a homogenous caspase assay kit [1]. |
Animal Research | In vivo, pharmacokinetic studies in female NCr athymic mice bearing WM266.4 human melanoma xenografts were essentially as described. NVP-AUY922 was dissolved in DMSO and diluted in sterile saline/Tween 20. A single dose of 50 mg/kg NVP-AUY922 was given i.v. or i.p. and groups of three animals were taken at intervals for pharmacokinetic analyses [1]. |
In vitro | 方法:HER2 阳性肿瘤细胞 OE19、ESO26、N87、OE33 和 SNU-216 用 Luminespib (1-1000 nM) 处理 72 h,通过 CellTiter-Glo luminescent cell viability assay 测定细胞活力。
结果:Luminespib 显示出强大的抗肿瘤效果,对 OE19、ESO26、N87、OE33 和 SNU-216 细胞的 IC50 分别为 20 nM、50 nM、80 nM、40 nM、50 nM。[1]
方法:HCT116 细胞用 Luminespib (80 nmol/L) 处理 8-72 h,通过 Western Blot 检测靶点蛋白表达水平。
结果:HCT116 细胞暴露于 Luminespib 导致 CRAF 和 ERBB2 的快速消耗以及伴随的 HSP72的诱导。[2] |
In vivo | 方法:为检测体内抗肿瘤活性,将 Luminespib (75-50 mg/kg) 腹腔注射给携带 WM266.4 异种移植物的 NCr athymic 小鼠,每天一次,持续 11 天。
结果:Luminespib 显著抑制了肿瘤生长速率,将对照组第 11 天的肿瘤平均重量从 252±19 mg 降低到 78±6 mg。第 11 天的肿瘤样本显示了耗竭 ERBB2 和 CDK4 的 HSP90 抑制特征,并诱导了 HSP72。[2] |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 16.67 mg/mL (35.8 mM) Ethanol : 29 mg/mL (62.3 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 8.6 mg/mL (18.47 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
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Keywords | VER 52296 | Inhibitor | HSP | AUY-922 | Autophagy | Heat shock proteins | VER52296 | Apoptosis | AUY 922 | inhibit | Luminespib | NVP-AUY 922 | NVP-AUY-922 |
Inhibitors Related | Guanidine hydrochloride | Naringin | Taurine | Gefitinib | Hydroxychloroquine | 5-Fluorouracil | Curcumin | Stavudine | Tributyrin | L-Ascorbic acid | Paeonol | Sodium 4-phenylbutyrate |
Related Compound Libraries | Inhibitor Library | Anti-Cancer Active Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | ReFRAME Related Library | Apoptosis Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |