| Identification | Back Directory | [Name]
LY900009 | [CAS]
209984-68-9 | [Synonyms]
LY900009
LY900009/LY-900009
7-(S)-(N'-((S)-(+)-2-hydroxy-3-methylbutyryl)-L-alaninyl)amino-5-methyl-5,7-dihydro-6H-dibenz[b,d]azepin-6-one
(2S)-2-hydroxy-3-methyl-N-[(2S)-1-[[(7S)-5-methyl-6-oxo-7H-benzo[d][1]benzazepin-7-yl]amino]-1-oxopropan-2-yl]butanamide
(S)-2-hydroxy-3-methyl-N-((S)-1-(((S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)amino)-1-oxopropan-2-yl)butanamide
Butanamide, N-[(1S)-2-[[(7S)-6,7-dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]amino]-1-methyl-2-oxoethyl]-2-hydroxy-3-methyl-, (2S)- | [Molecular Formula]
C23H27N3O4 | [MDL Number]
MFCD26142649 | [MOL File]
209984-68-9.mol | [Molecular Weight]
409.48 |
| Chemical Properties | Back Directory | [Boiling point ]
781.5±60.0 °C(Predicted) | [density ]
1.27±0.1 g/cm3(Predicted) | [solubility ]
DMSO mg/mL Water mg/mL Ethanol mg/mL | [form ]
Powder | [pka]
12.73±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
LY900009 is a potent and orally active, First-in-class inhibitor of Notch signaling via selective inhibition of the γ-secretase protein (GSI). LY900009 inhibits Notch signalling in tumor cell lines and endothelial cells (IC50=0.005-20 nM). LY900009 can be used for advanced cancer research[1]. | [in vivo]
LY900009 (oral gavage; 3 mg/kg; single dosage) revealed inhibition of angiogenesis through formation of leaky vasculature and produced tumour regression in Notch-dependent tumour models in a rat model[1]. | [target]
Notch | [References]
[1] Shubham Pant, et al. A first-in-human phase I study of the oral Notch inhibitor, LY900009, in patients with advanced cancer. Eur J Cancer. 2016 Mar;56:1-9. DOI:10.1016/j.ejca.2015.11.021 |
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