Powder: -20°C for 3 years | In solvent: -80°C for 1 year
NMS-E973 是一种有效且选择性的 Hsp90 抑制剂,与 Hsp90 结合的 DC50小于 10 nM。它能够穿越血脑屏障,具有抗肿瘤效果。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 327 | 现货 | ||
5 mg | ¥ 738 | 现货 | ||
10 mg | ¥ 1,230 | 现货 | ||
25 mg | ¥ 2,590 | 现货 | ||
50 mg | ¥ 3,790 | 现货 | ||
100 mg | ¥ 5,430 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 822 | 现货 |
产品描述 | NMS-E973 is a potent and selective Hsp90 inhibitor with DC50 of <10 nM for Hsp90 binding, no activiy against a panel of 52 diverse protein kinases. |
靶点活性 | HSP90:<10 nM(DC50) |
体外活性 | NMS-E973 shows a widespread antiproliferative activity with an average IC50 of 1.6 μM, and induces the degradation of client protein, such as Flt3, B-Raf, AKT, which further blocks tumor-related pathways, such as the Raf/MAPK, PI3K/AKT, and JAK/STAT pathways. [1] |
体内活性 | NMS-E973 (10 mg/kg i.v.) shows a favorable pharmacokinetic profile with selective retention in tumor tissue and ability to cross the BBB. NMS-E973 (60 mg/kg i.v.) shows high antitumor efficacy in all the models tested, including A375 and A2780 xenografts. In addition, NMS-E973 (10 mg/kg i.v.) together with B-Raf inhibitor PLX-4720 at 100 mg/kg produces a synergic anti-tumor effect. [1] In a mouse model of human ovarian cancer, NMS-E973 produces the antitumor activity by inhibition of Hsp90. [2] |
激酶实验 | Hsp90 binding assays: For competition experiments, a protein concentration of 5 nM for Hsp90 and of 200 nM for Trap1 are mixed with 0.5 nmol/L probe (final concentrations). After incubation, the dimethyl sulfoxide (DMSO) compound solution is added to the mixture. The plate is incubated for 18 hours at room temperature and then the fluorescence polarization signal was measured. Data are fitted with the program Dynafit version 3.28.039 or SigmaPlot (SSI) using the mathematical equation for competitive binding of 2 ligands to the receptor. |
分子量 | 454.43 |
分子式 | C22H22N4O7 |
CAS No. | 1253584-84-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 83 mg/mL (182.6 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2006 mL | 11.0028 mL | 22.0056 mL | 55.014 mL |
5 mM | 0.4401 mL | 2.2006 mL | 4.4011 mL | 11.0028 mL | |
10 mM | 0.2201 mL | 1.1003 mL | 2.2006 mL | 5.5014 mL | |
20 mM | 0.11 mL | 0.5501 mL | 1.1003 mL | 2.7507 mL | |
50 mM | 0.044 mL | 0.2201 mL | 0.4401 mL | 1.1003 mL | |
100 mM | 0.022 mL | 0.11 mL | 0.2201 mL | 0.5501 mL |
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。
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。
NMS-E973 1253584-84-7 Cytoskeletal Signaling Metabolism HSP NMS-E-973 Leukemia NMS E973 inhibit NMS-E 973 Heat shock proteins Adenocarcinoma Hsp90α ovary colon breast cancer Carcinoma Neuroblastoma NMSE973 Melanoma Inhibitor inhibitor