AP1903
| 中文名称 | AP1903 |
|---|---|
| 中文同义词 | (1R,1'R)-((((乙烷-1,2-二基双(氮二基))双(2-氧代乙烷-2,1-二基)双(氧基))-双(3,1-亚苯基))-(3-(3,4-二甲氧基苯基)丙烷-1,1-二基)(2S,2'S)-(1-((S)-2-(3,4,5-三甲氧基苯)丁酰基)哌啶-2-羧酸酯);利米多赛;AP 1903,蛋白质二聚化的化学诱导剂 |
| 英文名称 | AP1903 |
| 英文同义词 | AP1903;Rimiducid(AP1903);AP1903;RIMIDUCID;AP-1903;AP1903 (Rimiducid;CS-1237;RIMIDUCID;AP-1903;AP 1903;2-Piperidinecarboxylic acid, 1-[(2S)-1-oxo-2-(3,4,5-trimethoxyphenyl)butyl]-, 2,2'-[1,2-ethanediylbis[imino(2-oxo-2,1-ethanediyl)oxy-3,1-phenylene[(1R)-3-(3,4-dimethoxyphenyl)propylidene]]] ester, (2S,2'S)-;(1R,1'R)-((((Ethane-1,2-diylbis(azanediyl))bis(2-oxoethane-2,1-diyl))bis(oxy))bis(3,1-phenylene))bis(3-(3,4-dimethoxyphenyl)propane-1,1-diyl) (2S,2'S)-bis(1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate) |
| CAS号 | 195514-63-7 |
| 分子式 | C78H98N4O20 |
| 分子量 | 1411.63 |
| EINECS号 | 604-604-1 |
| 相关类别 | |
| Mol文件 | 195514-63-7.mol |
| 结构式 |  |
AP1903 性质
| 沸点 | 1307.5±65.0 °C(Predicted) |
|---|---|
| 密度 | 1?+-.0.06 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | DMSO:97.05(最大浓度 mg/mL);68.75(最大浓度 mM) 乙醇:120.58(最大浓度 mg/mL);85.42(最大浓度 mM) |
| 形态 | 固体 |
| 酸度系数(pKa) | 13.70±0.46(Predicted) |
EC50: 0.1 nM (FKBP, in HT1080 cells)
Fas receptor
The human fibrosarcoma line HT1080 is engineered to express stably a fusion protein comprising a myristoylation sequence, two copies of F36V-FKBP, and the human first apoptosis signal (Fas) intracellular domain. Rimiducid (AP1903) elicits potent and dose-dependent apoptotic death of these engineered cells in culture, with an EC 50 of ≈0.1 nM. Maximal killing occurred in the presence of 3 to 10 nM Rimiducid (AP1903), and the IC 50 is approximately 0.2 nM. LV′VFas-transduced T lymphocytes expressing high levels of CD25 (top panel) are eliminated by with 66%±7.5% (n=10) efficiency. When cells are examined after CD25 expression returned to basal levels, 63%±4.7% (n=9) killing is observed after Rimiducid treatment.
Rimiducid (AP1903; i.v.,0.01, 0.1, 1, 10, and 100 mg/kg) elicits a dose-dependent decrease in serum human GH levels, with a half-maximal effective dose of 0.4±0.1 mg/kg.