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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%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 368.47
Formula C19H16N2O2S2
CAS No. 1233948-35-0
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 73 mg/mL (198.11 mM)
Water: <1 mg/mL
Ethanol: 24 mg/mL (65.13 mM)
SMILES Code O=S(C1=CC=C(C)C=C1)(NC2=CC(C3=CC=C(C#N)S3)=CC=C2C)=O
Synonyms ELR-510444; ELR510444; ELR 510444.
实验参考方法
In Vitro

In vitro activity: ELR-510444 is a novel and potent inhibitor of microtubule polymeirzation (also called microtubule disruptor or mitotic inhibitor) with potential antivascular effects and in vivo antitumor efficacy, it can cause a loss of cellular microtubules and the formation of aberrant mitotic spindles which lead to mitotic arrest and apoptosis of cancer cells. ELR510444 also shows potent antitumor activity in the MDA-MB-231 xenograft model with at least a 2-fold therapeutic window. Studies in tumor endothelial cells show that a low concentration of ELR510444 (30 nM) rapidly alters endothelial cell shape, similar to the effect of the vascular disrupting agent combretastatin A4.


Kinase Assay: ELR510444 has potent microtubule-disrupting activity, causing a loss of cellular microtubules and the formation of aberrant mitotic spindles and leading to mitotic arrest and apoptosis of cancer cells.


Cell Assay: ELR510444 potently inhibits cell proliferation with an IC(50) value of 30.9 nM in MDA-MB-231 cells, inhibits the rate and extent of purified tubulin assembly, and displaces colchicine from tubulin, indicating that the drug directly interacts with tubulin at the colchicine-binding site. ELR510444 is not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines, suggesting that it circumvents both clinically relevant mechanisms of drug resistance to this class of agents.

In VivoELR510444 shows potent antitumor activity in the MDA-MB-231 xenograft model. A low concentration of ELR510444 (30 nM) rapidly alters endothelial cell shape
Animal model
Formulation & Dosage J Pharmacol Exp Ther. 2011 Mar;336(3):652-60.
References J Pharmacol Exp Ther. 2011 Mar;336(3):652-60.