WP1130

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WP1130

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:	856243-80-6
包装:	2mg, 5mg, 10mg, 50mg, 100mg

包装与价格：

产品名称

Degrasyn

产品介绍

Degrasyn (WP1130)是一种选择性的去泛素化酶(DUB: USP5， UCH-L1， USP9x， USP14， UCH37)抑制剂，也抑制Bcr/Abl，也是一种JAK2传感器(不影响20S蛋白酶体)和转录激活剂(STAT)。

细胞实验
细胞系	CML cells
方法	MTT (viability) assay CML cells were seeded in 96-well plates (2*104 cells/well) and WP1130, imatinib mesylate, or dasatinib (0.08-10 μ M) were added in a final volume of 100 μL medium. Plates were incubated at 37°C for 72 hours, after which 20 μL of 3-4,5-dimethylthiazolyl-2-2, 5-diphenyltetrazolium bromide (MTT) reagent (Sigma; stock 5 mg/mL) was added, and the plates were incubated at 37°C for another 2 hours. Cells were lysed with 100 L lysis buffer (20% sodium dodecyl sulfate [SDS] in 50% N, N-dimethylformamide adjusted to pH 4.7 with 80% acetic acid and 1 M hydrochloric acid; final concentration of acetic acid was 2.5% and hydrochloric acid was 2.5%) and incubated for 6 hours. The optical density of each sample at 570 nm was determined with a SPECTRA MAX M2 plate reader (Molecular Devices, Sunnyvale, CA).
浓度	0.08-10 μ M
处理时间	72 h

动物实验
动物模型	CML tumors and Bcr/Abl-expressing cells in nude mice
配制	a 0.1-mL suspension of 1:1 dimethylsulfoxide to polyethylene glycol 300
剂量	30 mg/kg every other day for 5 injections
给药处理	injected intraperitoneally

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	2.6021 mL	13.0107 mL	26.0213 mL
5 mM	0.5204 mL	2.6021 mL	5.2043 mL
10 mM	0.2602 mL	1.3011 mL	2.6021 mL