您好，欢迎来到化工原料网！ [登录] [免费注册]
化工原料网
发布求购
位置：首页 > 产品库 > NMS-E973
立即咨询
咨询类型：
     
*姓名：
*电话：
*单位：
Email：
*留言内容：
请详细说明您的需求。
*验证码：
 
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)
5mg电议
10mg电议

产品介绍
NMS-E973 是一种有效的选择性 HSP90 抑制剂。 NMS-E973 与 Hsp90α 的 ATP 结合位点结合，DC50<10 nM。 NMS-E973 能够穿过血脑屏障 (BBB)。抗肿瘤功效。
Cas No.1253584-84-7
Canonical SMILESCN1CCC(CC1)NC(=O)C2=CC(=C3C(=CC(=O)C=C3OC4=CC=C(C=C4)[N+](=O)[O-])O)ON2
分子式C22H22N4O7
分子量454.43
溶解度DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

NMS-E973 is a potent and selective inhibitor of heat shock protein 90 (Hsp90) with DC50 value of< 10nM [1].

Since Hsp90 plays an important role in the conformational maturation, stability and function of some oncogenic proteins, the inhibitors of Hsp90 are developed as therapeutic for cancers. NMS-E973 is a selective inhibitor of Hsp90. It binds to Hsp90α within the ATP binding site with DC50 value of< 10nM. Besides that, NMS-E973 shows no effect on a panel of 52 various protein kinases such as ABL, ACK1, AKT1 and Alk. The IC50 value of it for Hsc70 is >10μM. NMS-E973 exerts antiproliferation effects on A2780 tumor cell line and BT-474 breast cancer cell line with IC50 values of 69nM and 110nM, respectively. When treated with mice bearing A2780 xenografts, the intravenous administration of NMS-E973 significantly inhibits tumor growth with TGI value of 53% at dose of 30mg/kg. Moreover, NMS-E973 also displays antitumor activity in tumors resistant to kinase inhibitors such as vemurafenib [1, 2].

References:
[1] Brasca M G, Mantegani S, Amboldi N, et al. Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90). Bioorganic & medicinal chemistry, 2013, 21(22): 7047-7063.
[2] Fogliatto G, Gianellini L, Brasca M G, et al. NMS-E973, a novel synthetic inhibitor of Hsp90 with activity against multiple models of drug resistance to targeted agents, including intracranial metastases. Clinical Cancer Research, 2013, 19(13): 3520-3532.