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LY3039478

CAT: 0013-GTR19163260-01Size: 100 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19163260-01Size:100 mg
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Description
LY3039478 (Crenigacestat) is an exquisitely potent inhibitor of Notch-1 intracellular domain (N1ICD) cleavage with IC50 of 1 nM, also potently inhibits mutant Notch receptor activity; inhibits N1ICD cleavage and expression of Notch-regulated genes in the tumor microenvironment in xenograft tumor models; significantly inhibits the growth of CCRCC cell lines in a concentration-dependent manne, decreases expression of Myc and cyclin A1, causes G0/G1 cell cycle arrest in CCRCC cells, demonstrates in vivo efficacy in CCRCC in mice model. Blood Cancer Phase 2 Clinical (In Vitro) :Crenigacestat (100 nM) exhibits anti-cancer activity in K07074 cells (a primary mouse liver tumor cell line) .Crenigacestat (LY3039478) decreases expression of Myc and cyclin A1 (part of the NOTCH-driven proliferative signature) in murine and human model systems. Crenigacestat (LY3039478) treatment also leads to G0/G1 cell cycle arrest in CCRCC cells. (In Vivo) :Crenigacestat (8 mg/kg, oral gavage three times a week) resulted in significantly increases survival and delayed tumor growth in independent cohorts of mice demonstrating in vivo efficacy in CCRCC.
CAS Number
1421438-81-4
Product Name Alternative
Crenigacestat | LY 3039478
Purity
>98% (HPLC)
Solubility
DMSO: ≥ 34 mg/mL
Smiles
O=C (N[C@@H] (C) C (N[C@H]1C2=CC=CC=C2C3=CC=CN=C3N (CCO) C1=O) =O) CCC (F) (F) F
Molecular Formula
C22H23F3N4O4
Molecular Weight
464.4376
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
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-

Alternative Products

CatalogName
A4023-5LY3039478
S7169-01Crenigacestat (LY3039478)
A13544-100Crenigacestat (LY3039478) 100mg
A13544-50Crenigacestat (LY3039478) 50mg
A13544-10Crenigacestat (LY3039478) 10mg
A13544-25Crenigacestat (LY3039478) 25mg
A13544-1Crenigacestat (LY3039478) 1mg
A13544-5Crenigacestat (LY3039478) 5mg
A13544-10mM-DCrenigacestat (LY3039478) 10mM * 1mL in DMSO

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