AP1903

AP1903化学性质

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(Max Conc. mg/mL);68.75(Max Conc. mM)
Ethanol:120.58(Max Conc. mg/mL);85.42(Max Conc. mM)
形态 :A solid
酸度系数(pKa) :13.70±0.46(Predicted)
颜色 :White to light yellow

AP1903性质、用途与生产工艺

生物活性 Rimiducid (AP1903) 是二聚化剂，其通过交联 FKBP 结构域起作用，启动 Fas 信号传导，引起凋亡。Rimiducid (AP1903) 使 Caspase 9 自杀开关二聚化，并迅速诱导细胞凋亡 (apoptosis)。
靶点

EC50: 0.1 nM (FKBP, in HT1080 cells)
Fas receptor
体外研究

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.
体内研究

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.

AP1903上下游产品信息

上游原料

下游产品

AP1903生产厂家