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首页-小分子抑制剂&激动剂-Wnt/Notch/Hedgehog-Notch-LY3039478
LY3039478

Chemical Structure : LY3039478

CAS No.: 1421438-81-4

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LY3039478 (Crenigacestat;LY 3039478)

货号: 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.

规格 价格 库存 数量
5 mg ￥980 In stock
10 mg ￥1480 In stock
25 mg ￥2480 In stock
50 mg ￥3980 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 464.4376
分子式 C22H23F3N4O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 34 mg/mL
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-

参考文献

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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