BMS-906024 |
Katalog-Nr.GC35535 |
BMS-906024 ist ein oral aktiver und selektiver Inhibitor der γ-Sekretase (Gamma-Sekretase). BMS-906024 ist ein potenter pan-Notch-Rezeptor-Inhibitor mit IC50-Werten von 1,6 nM, 0,7 nM, 3,4 nM und 2,9 nM fÜr Notch1-, -2-, -3- bzw. -4-Rezeptoren. BMS-906024 zeigt eine antineoplastische BreitbandaktivitÄt.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1401066-79-2
Sample solution is provided at 25 µL, 10mM.
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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