| Identification | Back Directory | [Name]
BMS-906024 | [CAS]
1401066-79-2 | [Synonyms]
BMS-906024
BMS 906024,BMS906024
BMS-906024 >=98% (HPLC)
(2R,3S)-N1-((S)-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-2,3-bis(3,3,3-trifluoropropyl)succinamide
Butanediamide, N1-[(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)- | [Molecular Formula]
C26H26F6N4O3 | [MDL Number]
MFCD24849414 | [MOL File]
1401066-79-2.mol | [Molecular Weight]
556.5 |
| Hazard Information | Back Directory | [Uses]
BMS-906024 is an orally active and selective γ-secretase (gamma secretase) inhibitor. BMS-906024 is a potent pan-Notch receptors inhibitor with IC50s of 1.6 nM, 0.7 nM, 3.4 nM, and 2.9 nM for Notch1, -2, -3, and -4 receptors, respectively. BMS-906024 demonstrates broad-spectrum antineoplastic activity[1][2]. | [Definition]
ChEBI: (2S,3R)-N'-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-2,3-bis(3,3,3-trifluoropropyl)butanediamide is a primary carboxamide, a secondary carboxamide and a tertiary carboxamide. | [in vivo]
BMS-906024 (8.5 mg/kg; oral gavage; days 1 through 4 of each week for 3 weeks) significantly enhances the tumor growth inhibition of Paclitaxel (36 mg/kg). BMS-906024 enhances Paclitaxel-mediated cytotoxicity in vivo in NSCLC through a combination of inhibiting proliferation and promoting apoptosis, in a p21 and p57-independent manner[1].
BMS-906024 has a T1/2 of 4.6/5.3 hours, a Cmax of 1/0.3 μM and an AUC of 3.4/1.9 μM hour for IV/PO[2].
| Animal Model: | Six to 12-week-old female NOD scid gamma (NSG) mice with KRAS- and BRAF-WT PDX-T42 xenografts[1] | | Dosage: | 8.5 mg/kg | | Administration: | oral gavage; days 1 through 4 of each week for 3 weeks | | Result: | Significantly enhanced the tumor growth inhibition of Paclitaxel (36 mg/kg), but had no significant effect on Cisplatin (2 mg/kg) treatment.
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| Animal Model: | Mouse[2] | | Dosage: | 1 mg/kg (Pharmacokinetic Analysis) | | Administration: | IV or PO | | Result: | Had a T1/2 of 4.6/5.3 hours, a Cmax of 1/0.3 μM and an AUC of 3.4/1.9 μM?hour for IV/PO.
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| [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. DOI:10.1158/1535-7163.MCT-17-0439
[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. DOI:10.1021/acsmedchemlett.5b00001 |
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BOC Sciences
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