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10074-G5

Catalog No. T3686   CAS 413611-93-5

10074-G5 is an inhibitor of c-Myc-Max dimerization.

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10074-G5 Chemical Structure
10074-G5, CAS 413611-93-5
Pack Size Availability Price/USD Quantity
2 mg In stock $ 35.00
5 mg In stock $ 57.00
10 mg In stock $ 80.00
25 mg In stock $ 145.00
50 mg In stock $ 237.00
100 mg In stock $ 417.00
200 mg In stock $ 595.00
500 mg In stock $ 948.00
1 mL * 10 mM (in DMSO) In stock $ 63.00
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Purity: 99.67%
Purity: 97.22%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 10074-G5 is an inhibitor of c-Myc-Max dimerization.
Targets&IC50 c-Myc:2.8 μM(Kd)
In vitro 10074-G5 binds to and distorts the bHLH-ZIP domain of c-Myc, thereby inhibiting c-Myc/Max heterodimer formation and inhibiting its transcriptional activity. In vitro, 10074-G5 inhibits the growth of Daudi Burkitt's lymphoma cells and disrupts c-Myc/Max dimerization. Daudi cells accumulates 10074-G5, and the highest intracellular concentration is observed at 6 h. 10074-G5 inhibits c-Myc/Max dimerization in Daudi cells by approximately 75% at 4 h, and this inhibition is maintained through 24 h of incubation. Total c-Myc protein expression also decreases, and after 24 h exposure to 10 μM 10074-G5, c-Myc protein expression decreases approximately 40% compared with vehicle-treated control. 10074-G5 is cytotoxic in vitro against Daudi and HL-60 cells, which overexpress c-Myc [2].
In vivo The plasma half-life of 10074-G5 in mice treated with 20 mg/kg i.v. is 37 min, and peak plasma concentration is 58 μM, which is 10-fold higher than peak tumor concentration. The lack of antitumor activity probably is caused by the rapid metabolism of 10074-G5 to inactive metabolites, resulting in tumor concentrations of 10074-G5 insufficient to inhibit c-Myc/Max dimerization. Plasma 10074-G5 peak concentration (Cmax) of 58.5 ± 2.7 nmol/ml is observed at 5 min after intravenous administration of 20 mg/kg to mice bearing Daudi xenografts, 10074-G5 concentration in plasma declines rapidly. Except for lung, liver, and fat, tissue concentrations of 10074-G5 are lower than those of plasma at all time points[2].
Cell Research Daudi cells (3 × 108 cells in logarithmic growth) are incubated for 0, 1, 3, 6, or 24 h in 3 ml of complete medium containing 10 μM 10074-G5. After incubation, cells are harvested, split into two samples of 1.5 ml each, and overlaid in microcentrifuge tubes containing 0.5 ml of silicon oil. The tubes are centrifuged at 12,000 g for 4 min. After centrifugation, the top 1 ml of medium is removed and stored in cryovials at ?70°C until analysis. The remaining medium and silicon oil are carefully removed without disturbing the cell pellets. The sides of the tubes are cleaned with cotton-tipped applicators, and the cell pellets are stored at ?70°C until analysis.(Only for Reference)
Molecular Weight 332.31
Formula C18H12N4O3
CAS No. 413611-93-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 56 mg/mL (168.5 mM)

Ethanol: 10 mg/mL (30.09 mM)

TargetMolReferences and Literature

1. Yap JL, et al. Bioorg Med Chem Lett. 2013, 23(1):370-4. 2. Clausen DM, et al. J Pharmacol Exp Ther. 2010, 335(3):715-27.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Cancer Compound Library Autophagy Compound Library Cell Cycle Compound Library Target-Focused Phenotypic Screening Library Glutamine Metabolism Compound Library Apoptosis Compound Library Anti-Cancer Metabolism Compound Library Transcription Factor-Targeted Compound Library PPI Inhibitor Library

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Moracin D MYCi361 10058-F4 Coronarin D Mycro 3 c-Myc inhibitor 11 Aaptamine Nicotinamide N-oxide

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Keywords

10074-G5 413611-93-5 Autophagy Cell Cycle/Checkpoint c-Myc 10074G5 Inhibitor 10074 G5 10074-G-5 inhibit Myc inhibitor

 

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