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CAS号:66-76-2
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英文名称:Dicoumarol
分子式
C19H12O6
分子量
336
EINECS号
200-632-9
MDL
MFCD00006857
Smiles
C(C1=C(O)C2=CC=CC=C2OC1=O)C1=C(O)C2=CC=CC=C2OC1=O
InChIKey
DOBMPNYZJYQDGZ-UHFFFAOYSA-N
乙二醇化学百科
基本信息
物化性质
安全信息
生产及用途
Dicoumarol是一种竞争性的NADPH quinone oxidoreductase (NQO1)抑制剂,可通过干扰维生素K的代谢用作抗凝血剂。
Dicoumarol is an inhibitor of both NAD(P)H:quinone oxidoreductase 1 (NQO1) and PDK1 with IC 50 s of 0.37±0.15 and 19.42±0.032 μM, respectively. The PDK1 activity is inhibited by Dicoumarol in a dose-dependent manner. The enzymatic activity of PDK1 is reduced by approximately 94% when treated with 200 μM Dicoumarol. Dicoumarol decreases the p-PDHA1 level by 26% (100 μM Dicoumarol) and by 72% (200 μM Dicoumarol), with no statistical difference in the total PDHA1 level. Both 100 μM and 200 μM Dicoumarol markedly induce apoptosis of SKOV3 cells. Similarly, flow cytometric analysis of annexin V + PI + cells reveals that 100 μM and 200 μM Dicoumarol treatments generate approximately 20.87% and 24.94% apoptotic cells, respectively, significantly higher than vehicle treatment. It is also observed that treatment of MCF-7-TAMR cells with Dicoumarol, a known NQO1 inhibitor, reverses their tamoxifen-resistance phenotype.
Dichloroacetate (DCA) at 100 mg/kg, Dicoumarol at 30 mg/kg, and Dicoumarol at 50 mg/kg all significantly reduce tumor volume and decrease tumor weight, when compare to tumors from control or vehicle groups. Total caspase-3 and total anti-poly (ADP-ribose) polymerase (PARP) are significantly decreased in Dicoumarol-treated SKOV3 xenografts, when compare to tumors from the control or vehicle group.
类别 农药毒性分级 高毒急性毒性 口服- 大鼠 LD50: 250 毫克/ 公斤; 口服- 小鼠 LD50: 233 毫克/ 公斤可燃性危险特性 受热分解刺激烟雾;药物对生殖系统付作用:死胎,畸胎,婴儿不良;药物过量出血储运特性 库房通风低温干燥; 与食品原料分开储运灭火剂 干粉、泡沫、砂土
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