中文名 | GSK1324726A |
英文名 | GSK1324726A |
别名 | 化合物GSK1324726A BET蛋白抑制剂(GSK1324726A) 4-((2S,4R)-1-乙酰基-4-((4-氯苯基)氨基)-2-甲基-1,2,3,4-四氢喹啉-6-基)苯甲酸 4-[(2S,4R)-1-乙酰基-4-[(4-氯苯基)氨基]-2-甲基-1,2,3,4-四氢-6-喹啉基]苯甲酸 |
英文别名 | CS-1736 I-BET726 I-BET 726 GSK1324726A GSK1324726A (I-BET726) 4-(cis-1-Acetyl-4-((4-chlorophenyl)amino)-2-methyl-1,2,3,4-tetrahydroquinolin-6-yl)benzoic acid 4-((2S,4R)-1-acetyl-4-(4-chlorophenylamino)-2-methyl-1,2,3,4-tetrahydroquinolin-6-yl)benzoic acid 4-[(2S,4R)-1-Acetyl-4-[(4-chlorophenyl)amino]-2-methyl-1,2,3,4-tetrahydro-6-quinolinyl]benzoic acid 4-[(2S,4R)-1-Acetyl-4-[(4-chlorophenyl)amino]-1,2,3,4-tetrahydro-2-methyl-6-quinolinyl]benzoic acid |
CAS | 1300031-52-0 |
化学式 | C25H23ClN2O3 |
分子量 | 434.91 |
密度 | 1.304±0.06 g/cm3(Predicted) |
沸点 | 707.3±60.0 °C(Predicted) |
溶解度 | DMSO : ≥ 46 mg/mL (105.77 mM) |
酸度系数 | 4.20±0.10(Predicted) |
存储条件 | -20℃ |
靶点 | BRD2; BRD3; BRD4 |
体外研究 | In neuroblastoma cell lines, GSK1324726A inhibits cell growth and induces cytotoxicity. GSK1324726A also modulates expression of genes involved in apoptosis, signaling, and MYC-family pathways, including the direct suppression of BCL2 and MYCN. |
体内研究 | In the mouse SK–N-AS and CHP-212 models, GSK1324726A (15 mg/kg p.o.) results in tumor growth inhibition and down-regulation MYCN and BCL2 expression. In a mouse septic shock model, GSK1324726A (10 mg/kg i.v.) shows potent anti-inflammatory effects, and prevents death of diseased animals. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.299 ml | 11.497 ml | 22.993 ml |
5 mM | 0.46 ml | 2.299 ml | 4.599 ml |
10 mM | 0.23 ml | 1.15 ml | 2.299 ml |
5 mM | 0.046 ml | 0.23 ml | 0.46 ml |
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