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CAS No.: 1233948-35-0

ELR510444 Catalog No. CSN16317

Synonyms: ELR510444

ELR510444 is an inhibitor of tubulin polymerization with IC50 value of 10 μM.

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生物活性

实验方案

技术信息

生物活性

描述ELR510444 is a microtubule disruptor that inhibited the proliferation of MDA-MB-231 cells with an IC50 value of 30.9nM. It also exhibited inhibitory activity in MDA-MB-435 melanoma cells and 2H-11 tumor endothelial cells with IC50 values of 9.0±0.5 and 11.7±0.4nM, respectively. Compared with the parental HeLa cell line, ELR510444 showed an Rr value of 1.4 in βIII-expressing HeLa cells. ELR510444 treatment resulted in significant loss of interphase microtubules in A-10 cells with an EC₅₀ value of 21nM. Treatment of HeLa cells with 25nM ELR510444 for 18 h led to mitotic arrest and aberrant mitotic spindles. ELR510444 at 5 and 10μM inhibited the rate and extent of microtubule polymerization in a concentration-dependent manner, with 50% inhibition observed at a dosage of 10μM. ELR510444 also displaced colchicine from tubulin with a maximum displacement of 40% observed at 100μM. Oral administration of ELR510444 (3 and 6mg/kg) once daily for 28 days caused dose-dependent antitumor effects in an MDA-MB-231 xenograft model^[3].
作用机制ELR510444 is a potent microtubule disruptor that induces the formation of aberrant mitotic spindles and subsequent mitotic arrest and apoptotic cell death^[3].
参考文献

[1] Carew JS, Esquivel JA 2nd, et al. ELR510444 inhibits tumor growth and angiogenesis by abrogating HIF activity and disrupting microtubules in renal cell carcinoma. PLoS One. 2012;7(1):e31120.
[2] Risinger AL, Westbrook CD, et al. ELR510444, a novel microtubule disruptor with multiple mechanisms of action. J Pharmacol Exp Ther. 2011 Mar;336(3):652-60.
[3] Risinger AL, Westbrook CD, Encinas A, et al. ELR510444, a novel microtubule disruptor with multiple mechanisms of action. J Pharmacol Exp Ther. 2011;336(3):652-660.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7139 mL
- 13.5695 mL
- 27.1391 mL
- 5 mM
- 0.5428 mL
- 2.7139 mL
- 5.4278 mL
- 10 mM
- 0.2714 mL
- 1.3570 mL
- 2.7139 mL

技术信息

CAS号

1233948-35-0

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H16N2O2S2

运输

蓝冰

分子量

368.47

别名

ELR510444

溶解度

DMSO	120.0 mg/mL (325.7 mM) warming
Water	insoluble

动物实验配方

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