LY900009

Names

[ CAS No. ]:
209984-68-9

[ Name ]:
LY900009

[Synonym ]:
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)-
(2S)-2-Hydroxy-3-methyl-N-[(2S)-1-{[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]amino}-1-oxo-2-propanyl]butanamide
LY900009

Biological Activity

[Description]:

LY900009 is a potent and orally active, First-in-class inhibitor of Notch signaling via selective inhibition of the γ-secretase protein (GSI). LY900009 inhibited Notch signalling in tumor cell lines and endothelial cells (IC50 range: 0.005-20 nM). LY900009 can be used for advanced cancer research[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Stem Cell/Wnt >> Notch

[In Vivo]

在大鼠模型中，LY900009 (口服灌胃；3 mg/kg；单剂量) 通过形成渗漏脉管系统抑制血管生成，并在 Notch 依赖性肿瘤模型中导致肿瘤消退[1]。

[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.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
781.5±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₃H₂₇N₃O₄

[ Molecular Weight ]:
409.48

[ Flash Point ]:
426.5±32.9 °C

[ Exact Mass ]:
409.200165

[ LogP ]:
3.97

[ Vapour Pressure ]:
0.0±2.8 mmHg at 25°C

[ Index of Refraction ]:
1.622

[ Storage condition ]:
-20℃

Related Compounds

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