中文名 | Dimethylenastron |
英文名 | Dimethylenastron |
别名 | 化合物DIMETHYLENASTRON EG5抑制剂(DIMETHYLENASTRON) 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 |
英文别名 | enastron Dimethylenastron Eg5 Inhibitor III Eg5 Inhibitor III(Dimethylenastron) Dimethylenastron - Eg5 inhibitor III 2,3,4,6,7,8-Hexahydro-4-(3-hydroxyphenyl)-7,7-dimethyl-2-thioxo-5(1H)-quinazolinone 5(1H)-Quinazolinone, 2,3,4,6,7,8-hexahydro-4-(3-hydroxyphenyl)-7,7-dimethyl-2-thioxo- |
CAS | 863774-58-7 |
化学式 | C16H18N2O2S |
分子量 | 302.39 |
密度 | 1.34±0.1 g/cm3(Predicted) |
沸点 | 475.6±55.0 °C(Predicted) |
溶解度 | DMSO: 可溶15mg/mL,澄清 |
酸度系数 | 9.59±0.10(Predicted) |
存储条件 | 2-8°C |
外观 | 粉末 |
颜色 | white to beige |
体外研究 | Dimethylenastron is a potent Eg5 inhibitor, with an IC 50 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. |
体内研究 | 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. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.491 ml | 17.455 ml | 34.91 ml |
5 mM | 0.698 ml | 3.491 ml | 6.982 ml |
10 mM | 0.349 ml | 1.745 ml | 3.491 ml |
5 mM | 0.07 ml | 0.349 ml | 0.698 ml |
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