生物活性

Tofacitinib (CP-690550,Tasocitinib)是一种新型JAK3抑制剂，IC50为1 nM，作用于JAK2和JAK1选择性低20到100倍。CP-690550 是特定的口服JAK3抑制剂, 作用于JAK2 和 JAK1,效果分别低20和100倍。CP-690550 对30种其他激酶没有作用效果，平均IC50 > 3000 nM。CP-690,550抑制IL-2诱导的增殖，比作用于GM-CSF诱导的增殖效果强30倍。

化学数据

分子量	312.37
分子式	C16H20N6O
CAS号	477600-75-2
纯度	100.00%
溶解性（25°C）	DMSO ≥60 mg/mL
储存和运输条件	-20°C, sealed 常温运输及临时存放

实验操作来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）

细胞实验
细胞系	cytokine-dependent NK92 cell line
方法	(A) After cytokine starvation for 24 hours, NK92 cells were stimulated by the addition of human IL-2 for 48 hours with and without the addition of serially increasing concentrations of tofacitinib. 3H-thymidine was added during the last 6 hours of the cultures. Cells were then harvested and analyzed for 3H-thymidine incorporation. (B) Cytokine-starved NK92 cells were stimulated with human IL-2, combined IL-6/IL- 6R, or IL-12 for 48 hours with and without serially increasing concentrations of tofacitinib. (C) The NK92 cells were treated as those in panel B with and without a single 50nM dose of tofacitinib. Data are presented as means ±SD (A-C) and are representative of 3 independent experiments. (D) After cytokine starvation for 24 hours, NK92 cells were stimulated with 30 ng/mL of IL-2, 100 ng/mL of combined IL-6/IL-6R, or 100 ng/mL of IL-12 for 1 hour with and without the addition of tofacitinib. The cell lysates were immunoblotted with an anti–phospho-STAT5 monoclonal antibody and an anti-STAT5 antibody. ss-Actin was used as an input control. Data are representative of 3 independent experiments.
浓度	0~400 nM
处理时间	48 h

动物实验
动物模型	IL-15–transgenic CD8 T-cell leukemia–bearing mice
配制	dissolved in polyethylene glycol 300 (PEG300; VWR Scientific Products)
剂量	50 mg/mL
给药处理	continuously administered via a subcutaneous mini-osmotic pump (ALZET)

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

	小鼠	大鼠	兔	豚鼠	仓鼠	狗
重量 (kg)	0.02	0.15	1.8	0.4	0.08	10
体表面积 (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km系数	3	6	12	8	5	20

动物 A (mg/kg) = 动物 B (mg/kg) ×	动物 B的Km系数
	动物 A的Km系数

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

储备液配制

以下数据基于半岛bd体育手机客户端 分子量，对于特殊半岛bd体育手机客户端 ，请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.2013 mL	16.0067 mL	32.0133 mL
5 mM	0.6403 mL	3.2013 mL	6.4027 mL
10 mM	0.3201 mL	1.6007 mL	3.2013 mL