Dimethylenastron
目录号: PL14212 纯度: ≥98%
CAS No. :863774-58-7
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中文名称
Dimethylenastron
中文别名
2,3,4,6,7,8-六氢-4-(3-羟基苯基)-7,7-二甲基-2-硫代-5(1H)-喹唑啉酮;4-氨基-3-甲基苯甲酸乙酯
英文名称
Dimethylenastron
英文别名
5(1H)-Quinazolinone,2,3,4,6,7,8-hexahydro-4-(3-hydroxyphenyl)-7,7-dimethyl-2-thioxo-;Dimethylenastron;4-(3-hydroxyphenyl)-7,7-dimethyl-2-sulfanylidene-3,4,6,8-tetrahydro-1H-quinazolin-5-one;Dimethylnasetron;Eg5 Inhibitor III, Dimethylenastron;Rac-Dimethylenastron;2,3,4,6,7,8-Hexahydro-4-(3-hydroxyphenyl)-7,7-dimethyl-2-thioxo-5(1H)-quinazolinone;7,7-Dimethyl-4-(3-hydroxyphenyl)-5-oxo-3,4,5,6,7,8-hexahydroquinazolin-2(1H)-thione;Eg5 inhibitor III;AOB2736;SYN5065;BCP17179;AK548019;Eg5 Inhib
Cas No.
863774-58-7
分子式
C16H18N2O2S
分子量
302.39
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Dimethylenastron 是一种有效的驱动蛋白 Eg5 抑制剂,IC50 值为 200 nM。
生物活性
Dimethylenastron is a potent kinesin Eg5 inhibitor, with an IC 50 of 200 nM.
性状
Solid
IC50 & Target[1][2]
Eg5 200 nM (IC50)
体外研究(In Vitro)
Dimethylenastron is a potent Eg5 inhibitor, with an IC50 of 200 nM. Dimethylenastron exhibits no inhibition of five other kinesin subfamilies (kinesin 1/4/7/10 and one ungrouped-originating from 4 different organisms). Dimethylenastron (0.5, 1 μM) causes accumulation of cells in G2/M in HeLa cells. Dimethylenastron (3 and 10 μM) concentration-dependently suppresses the migratory ability of the cancer cells in PANC1 pancreatic cancer cells after treatment for 24 h, but does not inhibit the proliferation of cancer cells at 24 h until 72 h. Dimethylenastron also reduces invasion ability of the cancer cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Dimethylenastron (1.0 μmol) induces a milder scarring but the length of bleb survival is not significantly prolonged compared with the control group. Dimethylenastron (1.0 μmol) reveals a markedly reduced ratio of intraocular pressure and a milder, but not obviously reduced, subconjunctival fibrotic reaction in the rabbits treated with glaucoma filtration surgery. has not independently confirmed the accuracy of these methods. They are for reference only.
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]. Gartner M, et al. Development and biological evaluation of potent and specific inhibitors of mitotic Kinesin Eg5. Chembiochem. 2005 Jul;6(7):1173-7.
[2]. Sun XD, et al. Dimethylenastron suppresses human pancreatic cancer cell migration and invasion in vitro via allosteric inhibition of mitotic kinesin Eg5. Acta Pharmacol Sin. 2011 Dec;32(12):1543-8.
溶解度数据
In Vitro: DMSO : 100 mg/mL (330.70 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

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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