中文名 | Poloxin |
英文名 | Poloxin |
别名 | POLO-LIKE KINASE1(PLK1)抑制剂(POLOXIN) 2-甲基-5-(1-甲基乙基)-2,5-环己二烯-1,4-二酮 1-[O-(2-甲基苯甲酰)肟] |
英文别名 | Poloxin Polo-like Kinase Inhibitor V, Poloxin (Z)-2-Isopropyl-5-methyl-4-(((2-methylbenzoyl)oxy)imino)cyclohexa-2,5-dienone 2-Methyl-5-(1-methylethyl)-1-[O-(2-methylbenzoyl)oxime]-2,5-Cyclohexadiene-1,4-dione 2-Methyl-5-(1-methylethyl)-2,5-cyclohexadiene-1,4-dione 1-[O-(2-methylbenzoyl)oxime] 2,5-Cyclohexadiene-1,4-dione, 2-methyl-5-(1-methylethyl)-, 1-[O-(2-methylbenzoyl)oxime] |
CAS | 321688-88-4 |
化学式 | C18H19NO3 |
分子量 | 297.35 |
密度 | 1.11 |
沸点 | 418.6±55.0 °C(Predicted) |
溶解度 | DMSO: 可溶物5mg/mL (澄清溶液,温热) |
存储条件 | 2-8°C |
外观 | 黄色固体 |
颜色 | white to beige |
MDL号 | MFCD00534351 |
体外研究 | Poloxin (25 μM) induces defects in centrosome integrity, spindle formation, and chromosome alignment in mitosis. Centrosomal fragmentation induced by Poloxin is partially rescued by Kiz T379E. Poloxin (25 μM) activates the mitotic checkpoint, induces apoptosis and inhibits proliferation of MDA-MB-231 cells. Poloxin inhibits proliferation in both cell lines with a comparable efficiency through 72 h period. Poloxin inhibits the polo-box domain (PBD) interaction with an apparent IC 50 of ∼4.8 μM. Poloxin exhibits a loose Plk1 PBD specificity with 4-10 times higher IC 50 values for Plk2 and Plk3, and does not significantly inhibit other types of phosphopeptide-binding domains such as FHA, WW, and SH2 domains. |
体内研究 | Poloxin (40 mg/kg) decreases the proliferation of MDA-MB-231 cells, and surpresses the growth of the tumor nude mice bearing established xenografts of MDA-MB-231. |
危险品标志 | Xi - 刺激性物品 N - 危害环境的物品 |
风险术语 | R43 - 与皮肤接触可能致敏。 R50 - 对水生生物有极高毒性。 |
安全术语 | S36/37 - 穿戴适当的防护服和手套。 S61 - 避免释放至环境中。参考特别说明/安全数据说明书。 |
危险品运输编号 | UN 3077 9 / PGIII |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.363 ml | 16.815 ml | 33.63 ml |
5 mM | 0.673 ml | 3.363 ml | 6.726 ml |
10 mM | 0.336 ml | 1.682 ml | 3.363 ml |
5 mM | 0.067 ml | 0.336 ml | 0.673 ml |
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