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ELR510444
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ELR510444图片
CAS NO:1233948-35-0
规格:98%
分子量:368.47
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
Novel microtubule disruptor
CAS:1233948-35-0
分子式:C19H16N2O2S2
分子量:368.47
纯度:98%
存储:Store at -20°C

Background:

Microtubules are involved in nucleic and cell organization, division of intracellular structure, and intracellular transport, as well as ciliary and flagellar motility. Microtubule-targeting agents are some of the most effective chemotherapeutic drugs used in the clinic today. ELR510444 is a novel microtubule disruptor with multiple mechanisms of action.


In vitro: ELR510444 has potent microtubuledisrupting activity, causing a loss of intracellular microtubules and the formation of aberrant mitotic spindles and leading to mitotic arrest and apoptosis of cancer cells. ELR510444 inhibited cell proliferation, inhibited the rate and extent of purified tubulin assembly potently, and displaced colchicine from tubulin, revealing that the drug directly interacts with tubulin at the colchicine-binding site [1].


In vivo: ELR510444 also shows potent antitumor activity in the MDA-MB-231 xenograft model with at least a 2-fold therapeutic window [1].


Clinical trial: Up to now, ELR510444 is still in the preclinical development stage.


Reference:
[1] Risinger AL, Westbrook CD, Encinas A, Mülbaier M, Schultes CM, Wawro S, Lewis JD, Janssen B, Giles FJ, Mooberry SL.  ELR510444, a novel microtubule disruptor with multiple mechanisms of action. J Pharmacol Exp Ther. 2011 Mar;336(3):652-60.
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