價(jià)格 | 詢價(jià) |
包裝 | 5mg,10mg,20mg,50mg,100mg,200mg,500mg |
最小起訂量 | 5mg,10mg,20mg,50mg,100mg,200mg,500mg |
發(fā)貨地 | 廣東 |
更新日期 | 2023-06-02 |
中文名稱:MLN-4924 | 英文名稱:((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 | 產(chǎn)地: U.S.A |
保存條件: Room temperature, or -20oC for 2 year. | 純度規(guī)格: >99% by HPLC |
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:
成立日期 | 2016-04-01 (10年) | 注冊(cè)資本 | 100萬人民幣 |
員工人數(shù) | 10-50人 | 年?duì)I業(yè)額 | ¥ 100萬以內(nèi) |
主營(yíng)行業(yè) | 生物化工,化學(xué)試劑,醫(yī)藥原料 | 經(jīng)營(yíng)模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
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