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BMS-906024
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。
BMS-906024图片
CAS NO:1401066-79-2
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
BMS-906024 是一种口服有效,选择性的 γ 分泌酶 (gamma secretase) 抑制剂 (GSI),GSIs 是一类小分子 Notch 抑制剂。BMS-906024 可阻止具有高口服生物利用度的所有四种 Notch 受体的激活,对于 Notch1,-2,-3 和 -4 受体,IC50s 分别为 1.6,0.7,3.4 和 2.9 nM。 BMS-906024 表现出针对多种人癌症异种移植物的广谱抗肿瘤活性。
Cas No.1401066-79-2
Canonical SMILESO=C(N[C@@H]1C(N(C)C2=CC=CC=C2C(C3=CC=CC=C3)=N1)=O)[C@H](CCC(F)(F)F)[C@H](CCC(F)(F)F)C(N)=O
分子式C26H26F6N4O3
分子量556.5
溶解度Soluble in DMSO
储存条件Store at -20°C
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

BMS-906024 is an oral and selective gamma secretase inhibitor (GSI) that is a small molecule Notch inhibitor[1]. BMS-906024 prevents the activation of all four Notch receptors with a high oral bioavailability with IC50s of 1.6, 0.7, 3.4, and 2.9 nM for Notch1, -2, -3, and -4 receptors, respectively. BMS-906024 demonstrates broad-spectrum antineoplastic activity against a wide array of human cancer xenografts[2]. IC50: 1.6 nM (Notch1), 0.7 nM (Notch2), 3.4 nM (Notch3) and 2.9 nM (Notch4)[2]

[1]. Morgan KM, et al. Gamma Secretase Inhibition by BMS-906024 Enhances Efficacy of Paclitaxel in Lung Adenocarcinoma. Mol Cancer Ther. 2017 Dec;16(12):2759-2769. [2]. Gavai AV, et al. Discovery of Clinical Candidate BMS-906024: A Potent Pan-Notch Inhibitor for the Treatment of Leukemia and Solid Tumors. ACS Med Chem Lett. 2015 Mar 11;6(5):523-7.