5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
| 中文名称 | 5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione |
|---|---|
| 中文同义词 | 化合物ZLDI-8;5-((1-(2-(2,4-二甲基苯氧基)乙基)-2-甲基-1H-吲哚-3-基)亚甲基)-2-硫代二氢嘧啶-4,6(1H,5H)-二酮 |
| 英文名称 | 5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione |
| 英文同义词 | 5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione;IAC-8;pithelial-mesenchymal,ZLDI8,transition,anti-tumor,inhibit,Phosphatase,Sorafenib,E-Cadherin,N-Cadherin,Apoptosis,Notch,Survivin,ZLDI 8,Inhibitor,NICD,ADAM-17,cIAP1/2,Vimentin,ZLDI-8;4,6(1H,5H)-Pyrimidinedione, 5-[[1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl]methylene]dihydro-2-thioxo- |
| CAS号 | 667880-38-8 |
| 分子式 | C24H23N3O3S |
| 分子量 | 433.52 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 667880-38-8.mol |
| 结构式 | ![5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 结构式](CAS/20200119/GIF/667880-38-8.gif) |
5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 性质
| 密度 | 1.30±0.1 g/cm3(Predicted) |
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| 储存条件 | Store at -20°C |
| 溶解度 | 62.5 mg/mL，溶于 DMSO |
| 酸度系数(pKa) | 5.34±0.20(Predicted) |
| 形态 | 固体 |
| 颜色 | 黄至橙色 |
5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 用途与合成方法
ADAM-17
IC50: 31.6 μM (Tyrosine phosphatase)
Ki: 26.22 μM (Tyrosine phosphatase)
ZLDI-8 (0.03-30 μM; 6-72 hours; MHCC97-H cells) treatment reduces cell viability in a time- and dose-dependent manner.
ZLDI-8 (1-10 μM; 6-72 hours; MHCC97-H cells) significantly decreases the level of NICD and the accumulation of NICD in the nucleus. ZLDI-8 could also reduce the expression of pro-survival/anti-apoptosis regulators, Survivin and cIAP1/2. And also increases the expression of epithelial marker E-Cadherin and reduced mesenchymal markers N-Cadherin and Vimentin.
ZLDI-8 enhances chemotherapy effects on tumor cell proliferation blockage, induction of apoptosis and cell-cycle arrest by inhibiting Notch pathway and blocking chemical resistance.
Cell Viability Assay
| Cell Line: | MHCC97-H cells |
| Concentration: | 0.03 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, 30 μM |
| Incubation Time: | 6 hours, 12 hours, 24 hours, 48 hours, 72 hours |
| Result: | Emerged cytotoxic effect on MHCC97-H cells in a time- and dose-dependent manner. |
Western Blot Analysis
| Cell Line: | MHCC97-H cells |
| Concentration: | 1 μM, 3 μM, 10 μM |
| Incubation Time: | 6 hours, 12 hours, 24 hours, 48 hours, 72 hours |
| Result: | Significantly decreased the level of NICD and the accumulation of NICD in the nucleus. Also reduced the expression of pro-survival/anti-apoptosis regulators, Survivin and cIAP1/2 |
ZLDI-8 (0.2-2 mg/kg; intraperitoneal injection; every two days; for 20 days; nude mice) treatment enhances the effect of Sorafenib on inhibiting tumor growth in nude HCC-bearing mice model.
| Animal Model: | Nude mice with MHCC-97H cells |
| Dosage: | 2 mg/kg, 1 mg/kg, 500 μg/kg, or 200 μg/kg |
| Administration: | Intraperitoneal injection; every two days; for 20 days |
| Result: | Inhibited tumor growth in nude HCC-bearing mice model. |