[CAS NO. 413611-93-5] 10074-G5
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PRODUCTS SPECIFICATIONS [413611-93-5]
Catalog
SLK-S8426
Brand
Selleck
CAS
413611-93-5
DESCRIPTION [413611-93-5]
Overview
| MDL | MFCD00576774 |
|---|---|
| Molecular Weight | 332.31 |
| Molecular Formula | C18H12N4O3 |
| SMILES | O=[N+](C1=CC=C(NC2=CC=CC=C2C3=CC=CC=C3)C4=NON=C41)[O-] |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0092 mL | 15.0462 mL | 30.0924 mL |
| 5 mM | 0.6018 mL | 3.0092 mL | 6.0185 mL |
| 10 mM | 0.3009 mL | 1.5046 mL | 3.0092 mL |
| 50 mM | 0.0602 mL | 0.3009 mL | 0.6018 mL |
Description
10074-G5 is a inhibitor that binds to and distorts the bHLH-ZIP domain of c-Myc (Kd = 2.8 µM), thereby inhibiting c-Myc/Max heterodimer formation and inhibiting its transcriptional activity (IC50 = 146 µM).
Targets
| c-Myc [1] (Cell-free assay) |
| 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 .
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.
References
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