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WH-4-023

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Chemical Structure| 837422-57-8 同义名 : Dual LCK/SRC inhibitor;KIN001-112;KIN112
CAS号 : 837422-57-8
货号 : A135851
分子式 : C32H36N6O4
纯度 : 99%+
分子量 : 568.666
MDL号 : MFCD28138072
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(43.96 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

5% DMSO+30% PEG 300+5% Tween 80+water 1 mg/mL

生物活性
靶点

  • Src

    Src, IC50:6 nM

  • Lck

    Lck, IC50:2 nM

  • Cav 2.2

    Cav 2.2, IC50:0.001 μM

  • Calcium Channel

    Cav 2.2, IC50:0.001 μM
描述 WH-4-023 demonstrates comparable potency enhancement on Lck to that of 2-substituted variants[1].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
A498 cell Growth inhibition assay Inhibition of human A498 cell growth in a cell viability assay, IC50=0.18945 μM SANGER
COLO-829 cell Growth inhibition assay Inhibition of human COLO-829 cell growth in a cell viability assay, IC50=0.31212 μM SANGER
human A388 cell Growth inhibition assay Inhibition of human A388 cell growth in a cell viability assay, IC50=14.6758 μM SANGER
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.76mL

0.35mL

0.18mL

8.79mL

1.76mL

0.88mL

17.59mL

3.52mL

1.76mL
参考文献

[1]Martin MW, et al. Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity. J Med Chem. 2006 Aug 10;49(16):4981-91.