化合物TAS-116 T16994
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
5 mg | 1260533-36-5 | ¥617.00 | 询底价 |
10 mg | 1260533-36-5 | ¥987.00 | 询底价 |
50 mg | 1260533-36-5 | ¥2,950.00 | 询底价 |
1 mL | 1260533-36-5 | ¥685.00 | 询底价 |
1 mg | 1260533-36-5 | ¥269.00 | 询底价 |
100 mg | 1260533-36-5 | ¥4,350.00 | 询底价 |
25 mg | 1260533-36-5 | ¥1,980.00 | 询底价 |
Product Introduction
Bioactivity
英文名: Pimitespib
描述: Pimitespib (TAS-116) 是一种 ATP 竞争性和高度特异性的 HSP90α/HSP90β 抑制剂,Ki 值分别为 34.7 nM 和 21.3 nM。
体外活性: TAS-116 binds not only to the conventional-binding pockets as existing Hsp-90 inhibitors but also to a novel-binding pocket. Such a unique binding mode makes TAS-116 highly specific for Hsp-90α/β. TAS-116 (0-5 μM, 48 hours) inhibits human retinal pigment epithelial ARPE-19 cell lines and NCI-H929 MM cell growth. Compared 17-AAG in INA6 and NCI-H929 MM cells, more significant degradation of p-C-Raf and p-MEK1/2, HSP90 client proteins, and key RAS/RAF/MEK pathway regulators, is triggered by TAS-116 (0.125-1 μM, 24 hours) [2][3].
体内活性: TAS-116通过口服吸收,在小鼠中几乎具有100%的生物利用度,在大鼠中为69.0%。该化合物在小鼠(3.6 mg/kg, p.o.)、小鼠(7.1 mg/kg, p.o.)、小鼠(14.0 mg/kg, p.o.)、大鼠(4 mg/kg, p.o.)中的终末消除半衰期(t1/2)分别为8.2小时、2.5小时、4.4小时和2.2小时。相比其他HSP90抑制剂(t1/2=7.1-19.1小时),TAS-116在视网膜中的清除速度更快(t1/2=3.4小时),且在大鼠中主要分布在血浆而非视网膜,因此不引起可检测的感光细胞损伤。TAS-116能单独或与Bortezomib(BTZ)联合使用时增强体内抗多发性骨髓瘤(MM)活性,并展现出良好的安全性。TAS-116(12.0 mg/kg, p.o., 14天)显示出抗肿瘤活性而不引起大鼠眼部损伤。用TAS-116(10 mg/kg和15 mg/kg, 口服, 38天)、BTZ或TAS-116加BTZ治疗的小鼠,与对照组相比,显著增强了生长抑制。治疗组动物的中位总生存时间(TAS-116, 口服, 10 mg/kg=33天, 15 mg/kg=37天, BTZ=36天, 以及联合治疗=56.5天)显著长于对照组。TAS-116的有利药代动力学特征反映在其剂量依赖性的抗肿瘤活性上;T/C(TAS-116治疗的小鼠与对照组小鼠的肿瘤体积比)分别为3.6 mg/kg、7.1 mg/kg和14.0 mg/kg剂量时的47%、21%和9% [1][2]。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 125 mg/mL (275.01 mM)
关键字: inhibit | Pimitespib | HSP | TAS116 | TAS 116 | Heat shock proteins | Inhibitor
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相关库: Drug Repurposing Compound Library | Anti-Breast Cancer Compound Library | Anti-Cancer Drug Library | Anti-Metabolism Disease Compound Library | Bioactive Compounds Library Max | Endoplasmic Reticulum Stress Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Orally Active Compound 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