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。
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.
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