ELR510444|1233948-35-0|-陌孚医药/Medlife

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ELR510444

目录号: PL07205 纯度: ≥98.0%

CAS No. :1233948-35-0

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中文名称	ELR510444
中文别名	ELR510444 抑制剂;N-[5-(5-氰基-2-噻吩基)-2-甲基苯基]-4-甲基苯磺酰胺;ELR510444
英文名称	ELR510444
英文别名	ELR-510444;ELR510444;N-(5-(5-Cyanothiophen-2-yl)-2-methylphenyl)-4-methylbenzenesulfonamide;AOB6806;BCP13572;AK204430;BC600666;B5870;N-[5-(5-cyanothiophen-2-yl)-2-methylphenyl]-4-methylbenzene-1-sulfonamide;2-{4-[(E)-2-{5-[(1R)-1-(3,5-Dichloro-4-pyridinyl)ethoxy]-1H-indazol-3-yl}vinyl]-1H-pyrazol-1-yl}ethanol
Cas No.	1233948-35-0
分子式	C₁₉H₁₆N₂O₂S₂
分子量	368.47
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	ELR510444是新型微管阻断剂，抑制MDA-MB-231细胞增殖的IC50值为30.9nM，非P-gp底物分子。
生物活性	ELR510444 is a novel microtubule disruptor; inhibits MDA-MB-231 cell proliferation with IC50 of 30.9 nM; not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines. IC50 value: 30.9 nM(MDA-MB-231 cell) [1] Target: Microtubule disruptor 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. 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. ELR510444 is a novel microtubule-disr
性状	Solid
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Risinger AL, et al. ELR510444, a novel microtubule disruptor with multiple mechanisms of action. J Pharmacol Exp Ther. 2011 Mar;336(3):652-60. [2]. Carew JS, 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.

溶解度数据	In Vitro: DMSO : ≥ 37 mg/mL (100.42 mM)配制储备液

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2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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