CRENIGACESTAT

Name	LY3039478
Synonyms	LY3039478 LY 3039478 LY-3039478 Crenigacestat CRENIGACESTAT CRENIGACESTAT (LY3039478) 4-trifluoro-N-((S)-1-(((S)-5-(2-hydroxyethyl)-6-oxo-6 4,4,4-Trifluoro-N-((S)-1-(((S)-5-(2-hydroxyethyl)-6-oxo-6,7-dihydro-5H-benzo[d]pyrido[2,3-b]azepin-7-yl)amino)-1-oxopropan-2-yl)butanamide N-[(1S)-2-[[(7S)-6,7-Dihydro-5-(2-hydroxyethyl)-6-oxo-5H-pyrido[3,2-a][3]benzazepin-7-yl]amino]-1-methyl-2-oxoethyl]-4,4,4-trifluorobutanamide Butanamide, N-[(1S)-2-[[(7S)-6,7-dihydro-5-(2-hydroxyethyl)-6-oxo-5H-pyrido[3,2-a][3]benzazepin-7-yl]amino]-1-methyl-2-oxoethyl]-4,4,4-trifluoro-
CAS	1421438-81-4

Molecular Formula	C22H23F3N4O4
Molar Mass	464.44
Density	1.41±0.1 g/cm3(Predicted)
Boling Point	818.7±65.0 °C(Predicted)
Solubility	DMSO: ≥ 34 mg/mL
pKa	12.75±0.20(Predicted)
Storage Condition	-20℃
In vitro study	LY3039478 is a potent inhibitor of the cleavage of the intracellular region of Notch-1, with an IC50 of approximately 1 nM in most of the tumor cells examined. LY3039478 also potently inhibits mutant Notch receptor activity. LY3039478 significantly inhibited the growth of two renal clear cell carcinoma cells. Its treatment can reduce the expression of Myc and cyclin A1, causing cell arrest in G0/G1 phase of clear cell carcinoma cells.
In vivo study	In rats, its oral bioavailability was 65%,CL = 98 mL/min/kg, VDss = 4.9 L/kg. In dogs, the oral bioavailability was 67%,CL = 3.8 mL/min/kg, VDss = 1.4 L/kg. In xenograft tumor models, LY3039478 can inhibit the cleavage of N1ICD and the expression of Notch target genes in the tumor microenvironment. In a xenograft model that relies on Notch signaling, inhibition of Notch clipping induces apoptosis. In immunodeficient NSG-bearing mice (transplanted with 769-P CCRCC cells), LY3039478 significantly improved survival and delayed tumor growth.

Last Update：2024-01-02 23:10:35

Product Name: LY3039478 Visit Supplier Webpage Request for quotation
CAS: 1421438-81-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

Wechat: 18301782025

Product Name: LY3039478 Visit Supplier Webpage Request for quotation
CAS: 1421438-81-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

Wechat: 18301782025

View History

CRENIGACESTAT

CRENIGACESTAT Request for Quotation