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首页-小分子抑制剂&激动剂-Cytoskeleton/Cell Adhesion Molecules-Microtubule/Tubulin-ELR510444
ELR510444

Chemical Structure : ELR510444

CAS No.: 1233948-35-0

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ELR510444 (ELR-510444)

货号: PC-49251Not For Human Use, Lab Use Only.

ELR510444 (ELR-510444) is a small molecule microtubule disruptor that directly interacts with tubulin at the colchicine-binding site, shows potent microtubule-disrupting activity.

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25 mg ￥880 In stock
50 mg ￥1380 In stock
100 mg ￥2280 In stock
250 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

ELR510444 (ELR-510444) is a small molecule microtubule disruptor that directly interacts with tubulin at the colchicine-binding site, shows potent microtubule-disrupting activity.
ELR510444 treatment causes a loss of cellular microtubules and the formation of aberrant mitotic spindles and leading to mitotic arrest and apoptosis of cancer cells.
ELR510444 potently inhibited cell proliferation with an IC50 value of 30.9 nM in MDA-MB-231 cells, inhibited the rate and extent of purified tubulin assembly, and displaced colchicine from tubulin.
ELR510444 is not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines.
ELR510444 also shows potent antitumor activity in the MDA-MB-231 xenograft model with at least a 2-fold therapeutic window.
ELR510444 (30 nM) rapidly alters endothelial cell shape, similar to the effect of the vascular disrupting agent combretastatin A4

物理化学性质&存储条件

分子量 368.469
分子式 C19H16N2O2S2
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

10 mM in DMSO
Chemical Name/SMILES

N-[5-(5-cyano-2-thienyl)-2-methylphenyl]-4-methyl-benzenesulfonamide

参考文献

1. Risinger AL, et al. J Pharmacol Exp Ther. 2011 Mar;336(3):652-60.

2. Carew JS, et al. PLoS One. 2012;7(1):e31120.

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