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Chemical Structure : LY3039478
CAS No.: 1421438-81-4
Catalog No.: PC-43039Not For Human Use, Lab Use Only.
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $98 | In stock | |
| 10 mg | $148 | In stock | |
| 25 mg | $248 | In stock | |
| 50 mg | $398 | In stock | |
| 100 mg | Get quote |
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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.
LY3039478 inhibits N1ICD cleavage and expression of Notch-regulated genes in the tumor microenvironment in xenograft tumor models.
LY3039478 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.
LY3039478 demonstrates in vivo efficacy in CCRCC in mice model.
| M.Wt | 464.4376 | |
| Formula | C22H23F3N4O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: ≥ 34 mg/mL |
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| Chemical Name/SMILES |
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- |
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1. Bhagat TD, et al. J Biol Chem. 2017 Jan 20;292(3):837-846.
2. Cancer Discov. 2017 Feb;7(2):OF3. doi: 10.1158/2159-8290.CD-NB2016-159.
3. Mark H. Bender, et al. Abstract 1131: Novel inhibitor of Notch signaling for the treatment of cancer. DOI: 10.1158/1538-7445.AM2013-1131 Published April 2013
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