TG101209

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TG101209

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:	936091-14-4
包装:	5mg, 10mg, 25mg

包装与价格：

产品介绍

TG101209是一种选择性的JAK2抑制剂，IC50为6 nM，对Flt3和RET作用效果稍弱，IC50分别为25 nM和17 nM，作用于JAK2比作用于JAK3选择性高30倍左右，对JAK2V617F和MPLW515L/K突变型敏感。

细胞实验
细胞系	Ba/F3 cells, MPLW515L, CTLL-2 cells and HEL and K562 cells
方法	XTT assay for cell proliferation. In brief, approximately 2*10³cells were plated into microtiterplate wells in 100 ml RPMI-1640 growth media with indicated concentrations of inhibitor. The relative growth of cells was quantified at 24-h intervals using Cell Proliferation Kit II (XTT) as per manufacturer’s guidelines (Roche, Indianapolis, IN, USA). After incubation, 20 ml of XTT was added to the wells and allowed to incubate for 4–6 h. The colored formazan product was measured spectrophotometrically at 450 nm with correction at 650 nm, and IC50 values were determined using the GraphPad Prism 4.0 software. Data were subjected to a non-linear regression-fit analysis and IC50 values were determined as the concentration, that inhibited proliferation by 50%. All experiments were done in triplicate and the results normalized to growth of untreated cells.
浓度	0~100 μ M
处理时间	24 h

动物实验
动物模型	JAK2V617F-induced hematopoietic disease in a nude mouse model
配制	DMSO
剂量	10, 30 and 100mg/kg bid
给药处理	oral gavage

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

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。

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.9621 mL	9.8103 mL	19.6205 mL
5 mM	0.3924 mL	1.9621 mL	3.9241 mL
10 mM	0.1962 mL	0.981 mL	1.9621 mL