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BMS-906024

Names

[ CAS No. ]:
1401066-79-2

[ Name ]:
BMS-906024

[Synonym ]:
UNII-DRL23N424R
T67 GNVJN IHJ G1 IMVY2XFFFY2XFFFVZ KR &&(2R,3S)-(3S)- Form
(2R,3S)-N-((3S)-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)-2,3-bis(3,3,3-trifluoropropyl)succinamide
BMS-906024
Butanediamide, N-[(3S)-2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-2,3-bis(3,3,3-trifluoropropyl)-, (2R,3S)-
(2R,3S)-N-[(3S)-1-Methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl]-2,3-bis(3,3,3-trifluoropropyl)succinamide

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Stem Cell/Wnt >> Notch

[Target]

IC50: 1.6 nM (Notch1), 0.7 nM (Notch2), 3.4 nM (Notch3) and 2.9 nM (Notch4)[2]


[References]

[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.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
726.3±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C26H26F6N4O3

[ Molecular Weight ]:
556.500

[ Flash Point ]:
393.0±32.9 °C

[ Exact Mass ]:
556.190918

[ PSA ]:
109.34000

[ LogP ]:
2.10

[ Vapour Pressure ]:
0.0±2.4 mmHg at 25°C

[ Index of Refraction ]:
1.558

Related Compounds

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