产品详情
中文名称:MLN-4924 | 英文名称:((1S,2S,4R)-4-(4-(((S)-2,3-dihydro-1H-inden-1-yl)amino)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-2-hydroxycyclopentyl)methyl sulfamate |
CAS:905579-51-3 | 有效期: 一年 |
品牌: Activebiochem | 产地: U.S.A |
保存条件: Room temperature, or -20ºC for 2 year. | 纯度规格: >99% by HPLC |
2023-06-02
MLN-4924
((1S,2S,4R)-4-(4-(((S)-2,3-dihydro-1H-inden-1-yl)amino)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-2-hydroxycyclopentyl)methyl sulfamate
RMB
一年
Activebiochem
U.S.A
Room temperature, or -20ºC for 2 year.
>99% by HPLC
Biological Activity
MLN4924 is a first-in-class cancer drug that inhibits the Nedd8-activating enzyme (NAE).
In vivo administration of MLN4924 to mice bearing xenograft tumors of OCI-Ly10 and OCI-Ly19 resulted in a pharmacodynamic response of NAE pathway inhibition. In both models, a single dose of MLN4924 resulted in time and dose-dependent inhibition of total neddylated cullin levels and stabilization of CDL substrates including the CDL3Keap1 substrate, Nrf-2. Notably, in the OCI-Ly10 model, a single dose of MLN4924 resulted in a marked elevation of pIkBa levels, indicative of NF-kB pathway inhibition, and induction of apoptosis. In both OCI-Ly10 and OCI-Ly19 xenograft models, inhibition of the NAE pathway following repeated daily and intermittent dosing of MLN4924 translated into significant tumor growth inhibition. In the OCI-Ly10 model tumor regressions were observed showing this model to be particularly sensitive to MLN4924 treatment, reflecting the addiction of these tumors to NF-kB signaling. Additionally we demonstrate an inhibition of the NAE pathway and NF-KB signaling in a primary human tumor DLBCL xenograft model (PHTX-22L) resulting in tumor regressions following MLN4924 treatment. In summary, in tumors dependent on NF-kB signaling for growth and survival, MLN4924 inhibition of CDL activity provides a novel mechanism for targeted NF-kB pathway modulation and therapeutic intervention. In addition, these data demonstrate that MLN4924 is a novel agent that has broad activity in pre-clinical models of lymphoma. (source: Michael Milhollen, Usha Narayanan*, Allison J Berger, Michael Thomas, Tary Traore, Jie Yu, Julie Zhang, Erik Koenig, James J. Garnsey, Steven P. Langston, Teresa A Soucy, and Peter G Smith, MLN4924, a Novel Small Molecule Inhibitor of Nedd8-Activating Enzyme, Demonstrates Potent Anti-Tumor Activity in Diffuse Large B-Cell Lymphom, 50th ASH Annual Meeting and Exposition, or see website:
关键字: MLN-4924;MLN4924;4924
公司简介
专业生物试剂代理商.主要代理Sigma-Aldrich, ChemieTek, Active Biochem, Enzo LifeScience, Biomyx, Chemdea, Santa Cruz, Biolegend, BD Biosciences,Progmega, R&D Systems等美国品牌产品 ,是一家致力于主要遗传学过程的研究工具,诊断,治疗和相关医学团体实验室服务的领先生命科学与生物技术公司。
成立日期 |
2016-04-01
(9年)
|
注册资本 |
100万人民币
|
员工人数 |
10-50人 |
年营业额 |
¥ 100万以内 |
主营行业 |
生物化工,化学试剂,医药原料 |
经营模式 |
贸易,工厂,试剂,定制,服务 |