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10074-G5 {[allProObj[0].p_purity_real_show]}

货号:A188479

10074-G5是c-Myc-Max二聚化抑制剂,IC50值为146 μM,可与c-Myc的bHLH-ZIP区域结合使其变性。

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Type HazMat fee for 500 gram (Estimated)
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10074-G5 化学结构 CAS号:413611-93-5
10074-G5 化学结构
CAS号:413611-93-5
10074-G5 3D分子结构
CAS号:413611-93-5
10074-G5 化学结构 CAS号:413611-93-5
10074-G5 3D分子结构 CAS号:413611-93-5
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10074-G5 纯度/质量文件 产品仅供科研

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10074-G5 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].

10074-G5 细胞研究

细胞系 浓度 检测类型 检测时间 活性说明 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

10074-G5 动物研究

Animal study In mice administered an intravenous dose of 20 mg/kg of 10074-G5, the plasma half-life is recorded at 37 minutes. The peak plasma concentration reaches 58 μM, a level that is ten times greater than the highest concentration found in tumors[1].
Pharmacokinetics
Animal Mice[4]
Dose 20 mg/kg
Administration i.v.
Cmax 58.5 ± 2.7 nmol/ml
T1/2 37 min
CL 69 ml/min/kg
Vd 3000 ml/kg

10074-G5 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.

10074-G5 实验方案

计算器
存储液制备 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

10074-G5 技术信息

CAS号413611-93-5
分子式C18H12N4O3
分子量 332.313
别名
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place,Sealed in dry,Room Temperature

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方
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