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Chemical compound
BMS-906024
(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
CAS Number
PubChem
CID PubChem
SID
ChemSpider
UNII
CompTox Dashboard (
EPA )
Formula C 26 H 26 F 6 N 4 O 3
Molar mass 556.509 g·mol−1 3D model (
JSmol )
CN1c2ccccc2C(=N[C@@H](C1=O)NC(=O)[C@H](CCC(F)(F)F)[C@H](CCC(F)(F)F)C(=O)N)c3ccccc3
InChI=1S/C26H26F6N4O3/c1-36-19-10-6-5-9-18(19)20(15-7-3-2-4-8-15)34-22(24(36)39)35-23(38)17(12-14-26(30,31)32)16(21(33)37)11-13-25(27,28)29/h2-10,16-17,22H,11-14H2,1H3,(H2,33,37)(H,35,38)/t16-,17+,22+/m0/s1
Key:AYOUDDAETNMCBW-GSHUGGBRSA-N
BMS-906024 is a drug with a
benzodiazepine structure, developed by
Bristol-Myers Squibb and disclosed at the spring 2013
American Chemical Society meeting in New Orleans to treat breast, lung, colon cancers and leukemia.
[1] The drug works as a pan-
Notch inhibitor. The structure is one of a set patented in 2012,
[2] and is being studied in clinical trials.
[3]
[4]
[5]
References
^ Drahl C (2013).
"Liveblogging First-Time Disclosures of Drug Structures from #ACSNOLA" . Chemical and Engineering News . American Chemical Society.
^
WO 2012129353 , Quesnelle C, Kim SH, Lee F, Gavai A, "Bisfluoroalkyl-1,4-Benzodiazepinone Compounds", published 27 September 2012, assigned to Bristol-Myers Squibb Company
^ Gavai AV, Quesnelle C, Norris D, Han WC, Gill P, Shan W, et al. (May 2015).
"Discovery of Clinical Candidate BMS-906024: A Potent Pan-Notch Inhibitor for the Treatment of Leukemia and Solid Tumors" . ACS Medicinal Chemistry Letters . 6 (5): 523–7.
doi :
10.1021/acsmedchemlett.5b00001 .
PMC
4434460 .
PMID
26005526 .
^ Morgan KM, Fischer BS, Lee FY, Shah JJ, Bertino JR, Rosenfeld J, et al. (December 2017).
"Gamma Secretase Inhibition by BMS-906024 Enhances Efficacy of Paclitaxel in Lung Adenocarcinoma" . Molecular Cancer Therapeutics . 16 (12): 2759–2769.
doi :
10.1158/1535-7163.MCT-17-0439 .
PMC
5716926 .
PMID
28978720 .
^ Sosa Iglesias V, Theys J, Groot AJ, Barbeau LM, Lemmens A, Yaromina A, et al. (2018).
"Synergistic Effects of NOTCH/γ-Secretase Inhibition and Standard of Care Treatment Modalities in Non-small Cell Lung Cancer Cells" . Frontiers in Oncology . 8 : 460.
doi :
10.3389/fonc.2018.00460 .
PMC
6234899 .
PMID
30464927 .