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10074-G5

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Chemical Structure| 413611-93-5 同义名 : -
CAS号 : 413611-93-5
货号 : A188479
分子式 : C18H12N4O3
纯度 : 98%
分子量 : 332.313
MDL号 : MFCD00576774
存储条件：

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(90.28 mM)，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：
生物活性
描述 10074-G5 is effective in hindering the proliferation of Daudi Burkitt's lymphoma cells and in interfering with the dimerization of c-Myc/Max. It exhibits IC50 values of 15.6 μM for Daudi cells and 13.5 μM for HL-60 cells[1]. 10074-G5 interacts with the Myc peptide Myc353-437, exhibiting a Kd value of 2.8 μM within the Arg363-Ile381 region. It attaches within a pocket formed by a bend (Asp379-Ile381) at the N-terminal end of an induced helical segment (Leu370–Arg378)[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
Daudi cells Cytotoxicity assay 3 to 5 days Cytotoxicity against human Daudi cells assessed as growth inhibition after 3 to 5 days by MTT assay, IC50=10 Μm 23177256
HL60 cells Cytotoxicity assay 3 to 5 days Cytotoxicity against human HL60 cells assessed as growth inhibition after 3 to 5 days by MTT assay, IC50=30 μM 23177256
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.01mL

0.60mL

0.30mL

15.05mL

3.01mL

1.50mL

30.09mL

6.02mL

3.01mL
参考文献

[1]Clausen DM, et al. In vitro cytotoxicity and in vivo efficacy, pharmacokinetics, and metabolism of 10074-G5, a novel small-molecule inhibitor of c-Myc/Max dimerization. J Pharmacol Exp Ther. 2010 Dec;335(3):715-27.

[2]Yap JL, et al. Pharmacophore identification of c-Myc inhibitor 10074-G5. Bioorg Med Chem Lett. 2013 Jan 1;23(1):370-4.