AP1903
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) |
| 颜色 | 白色至浅黄色 |
| InChIKey | GQLCLPLEEOUJQC-ZTQDTCGGSA-N |
AP1903 用途与合成方法
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.
