| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
Onalespib 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。
产品描述 | Onalespib is a synthetic, orally bioavailable, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Onalespib selectively binds to Hsp90, thereby inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding, stability and degradation of many oncogenic signaling proteins. |
靶点活性 | Hsp90(AT13387):18 nM |
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。 |
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 |
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) |
别名 | AT13387, Onalespib (AT13387) |
分子量 | 409.53 |
分子式 | C24H31N3O3 |
CAS No. | 912999-49-6 |
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
DMSO: 33 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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。
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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。
Onalespib 912999-49-6 Cytoskeletal Signaling Metabolism HSP Heat shock proteins AT 13387 inhibit Inhibitor AT13387 Onalespib (AT13387) AT-13387 inhibitor