化合物Onalespib T6284

Product Introduction
Bioactivity


英文名: Onalespib

描述: Onalespib (AT13387) 是一种合成的、口服生物可利用的热休克蛋白 90 (Hsp90) 小分子抑制剂，Kd 值为 0.71 nM。具有潜在的抗肿瘤活性。它选择性地与 Hsp90 结合，从而抑制其伴侣功能并促进参与肿瘤细胞增殖和存活的致癌信号蛋白的降解。

细胞实验: The human cell lines including A375, 22RV1, T474, DU1 45, LNCa P, MCF-7, DA-MB-468 are seeded into 96-well plates before the addition of AT13387 in 0.1% (v/v) DMSO. GI50 are determined using a 10-point dose response curve for three cell doubling times. After AT13387 incubation 10% (v/v), Alamar blueis added, and cells are incubated for a further 4 hours. Fluorescence is read.(Only for Reference)

激酶实验: HSP90 competition isothermal calorimetry: Kd values for AT13387 binding to HSP90 are determined with a competition Isothermal Calorimetry (ITC) format. ITC experiments are performed on a Micro Cal VP-ITC at 25 °C in a buffer comprising 25 mM Tris, 100 mM NaCl, 1 mM MgCl2 and 1 mM Tris(2-carboxy- ethyl)phosphine at pH 7.4 in order to maintain the higher affinit

体外活性: 当间歇给药时,AT13387耐受剂量高达70 mg/kg每周两次或90 mg/kg每周一次.在两种给药方案中,NCI-H1975的肿瘤生长抑制是相似的.

体内活性: AT13387是来自多种不同肿瘤类型的许多不同细胞系（例如MES-SA细胞系）的增殖和存活的有效抑制剂。在一组30个肿瘤细胞系中,AT13387有效抑制细胞增殖,GI50值在13-260 nM范围内。 AT13387抑制非致瘤性人前列腺上皮细胞系PNT2的增殖,GI50值为480 nM。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 4.1 mg/mL (10 mM)


关键字: Onalespib | HSP | Heat shock proteins | inhibit | Inhibitor | AT-13387 | AT 13387

相关产品: HSP90-IN-27 | Col003 | AT-533 | Grp94 Inhibitor-1 | HA15 | PROTAC Hsp90α degrader 1 | NDNA3 | CCT018159 | GRP78-IN-3 | TRAP1-IN-1

相关库: Anti-Aging Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Metabolism Compound Library | Target-Focused Phenotypic Screening Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途