生物活�?/h4>

ZSTK474能够抑制I型PI3K亚型，IC50�?7 nM，对PI3Kδ作用最显著、�/p>

化学数据

分子野�/td>	417.41
分子弎�/td>	C19H21F2N7O2
CAS叶�/td>	475110-96-4
纯度	>98%
溶解性（25��C（�/td>	DMSO 20 mg/mL
储存和运输条仵�/td>	固体粉末� -20��C 冷藏长期储存 常温运输及临时存攽�/td>

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
细胞糺�/td>	panel of 39 human cancer cell lines
方法	Analysis of Cell Proliferation Inhibition The inhibition of cell proliferation was assessed by measuring changes in total cellular protein in a culture of each cell line in the JFCR panel of cell lines after 48 hours of drug treatment by use of a sulforhodamine B assay. The 50% growth inhibition (GI 50 ) value of the drug was calculated as described previously. The graphic representation of a drug’s mean differential growth inhibition for the cell line panel was based on a calcula-tion that used a set of GI 50 values, as described previously. To analyze the correlation between the mean graphs of drug A and drug B, the COMPARE computer algorithm was developed as previously described by Paull et al. The Pearson correla-tion coeffi cient between the mean graphs of drug A and drug B was calculated (n = 39).
浓度	0~10μM
处理时间	48 h

动物实验
动物模型	Human A549 lung cancer cells, PC-3 prostate cancer cells, and WiDr colon cancer cells tumor xenografts
配制	5% hydroxypropylcellulose in water
剂量	100, 200, or 400 mg/kg daily from days 0 to 13
给药处理	orally

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（�/h4>

	小鼠	大鼠	兓�/td>	豚鼠	仓鼠	狖�/td>
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�?），再除以大鼠的K_m系数�?），得到化合物用于大鼠的等效剂量�?0 mg/kg、�/p>

储备液配刵�/h4>

以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作、�/p>

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.3957 mL	11.9786 mL	23.9573 mL
5 mM	0.4791 mL	2.3957 mL	4.7915 mL
10 mM	0.2396 mL	1.1979 mL	2.3957 mL