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CAS No.: 413611-93-5

10074-G5 Catalog No. CSN20454

Synonyms: 10074-G5

10074-G5 is a c-Myc Max interaction inhibitor.

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生物活性

实验方案

技术信息

生物活性

描述C-Myc is helix–loop–helix–leucine zipper (HLH–ZIP) oncoprotein that is frequently deregulated in human cancers. 10058-F4 is an inhibitor of c-Myc through disruption of c-Myc-Max dimerization with Kd value of 2.8μM. 100μM 10074-G5 exhibited about 40% disruption of the Myc–Max dimer in EMSA assay. Significant apoptosis could be observed in both Rat1a and Rat1a-c-Myc cells exposure to 32μM 10074-G5 for 6 and 7 days, but not c-Myc KO cells. Treatment with 32μM 10074-G5 inhibited ornithine decarboxylase expression, a direct and positive c-Myc target, induced by 4-hydroxytamoxifen at 16h in Rat1a-MycER cells, and decreased c-Myc–Max-mediated transactivation in C3H10T1/2 cells transiently transfected with c-Myc and Max expression vectors with additional 48-hour treatment in cell lysis. Treatment with 10074-G5 for 72h exhibited dose-dependent antiproliferation in Daudi cells and HL-60 cells with IC50 values of 15.6μM and 13.5μM, respectively. However, lack of antitumor by 10074-G5 was found in vivo probably due to the rapid metabolism of 10074-G5 to inactive metabolites.
作用机制10074-G5 can disrupt the dimeric complex formed between its basic helix-loop-helix leucine zipper (bHLHZip) domain and a similar domain on its dimerization partner, Max. Similar to 10058-F4, 10074-G5 binds to c-Myc, but a distinct region^[1]. ^[1] ^[2] ^[3] ^[4] ^[5]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

动物研究
剂量
Mice^[4] (i.v.): 20 mg/kg

给药途径
i.v.

动物药代数据
Animal Mice^[4]
Dose 20 mg/kg
Administration i.v.
C_max 58.5 ± 2.7 nmol/ml
T_1/2 37 min
CL 69 ml/min/kg
V_d 3000 ml/kg
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0092 mL
- 15.0461 mL
- 30.0921 mL
- 5 mM
- 0.6018 mL
- 3.0092 mL
- 6.0184 mL
- 10 mM
- 0.3009 mL
- 1.5046 mL
- 3.0092 mL

技术信息

CAS号

413611-93-5

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H12N4O3

运输

蓝冰

分子量

332.31

别名

10074-G5

溶解度

DMSO	66.0 mg/mL (198.6 mM)
Water	Insoluble
Ethanol	10.0 mg/mL (30.1 mM) warming

动物实验配方

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