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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。
WP1130图片
CAS NO:856243-80-6
包装:2mg, 5mg, 10mg, 50mg, 100mg
包装与价格:
包装价格(元)
Free Sample (0.5-1 mg)电议
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品名称
Degrasyn
产品介绍

生物活性

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)。


化学数据

分子量384.3
分子式C19H18BrN3O
CAS号856243-80-6
纯度98.94%
溶解性(25°C)DMSO 60 mg/mL
储存和运输条件固体粉末: -20°C 冷藏长期储存
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

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)

小鼠大鼠豚鼠仓鼠
重量 (kg)0.020.151.80.40.0810
体表面积 (m2)0.0070.0250.150.050.020.5
Km系数36128520
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Km系数(3),再除以大鼠的Km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 / Mass1 mg5 mg10 mg
1 mM2.6021 mL13.0107 mL26.0213 mL
5 mM0.5204 mL2.6021 mL5.2043 mL
10 mM0.2602 mL1.3011 mL2.6021 mL