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NMS-E973
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NMS-E973图片
CAS NO:1253584-84-7
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议

产品介绍
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。

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.

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.

Cas No.

1253584-84-7

分子式

C22H22N4O7

分子量

454.439

储存和溶解度

DMSO:83 mg/mL (182.6 mM)
H2O:<1 mgml
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years