10074-G5

Catalog No.S8426 Batch:S842601

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Technical Data

Formula

C18H12N4O3
Molecular Weight 332.31 CAS No. 413611-93-5
Solubility (25°C)* In vitro DMSO 66 mg/mL (198.6 mM)
Ethanol 10 mg/mL (30.09 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description 10074-G5 is a c-Myc 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 [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].

Protocol (from reference)

Cell Assay:[2]
  • Cell lines

    Daudi cells

  • Concentrations

    10 μM

  • Incubation Time

    0, 1, 3, 6, or 24 h

  • Method

    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 12,000g 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.
Animal Study:[2]
  • Animal Models

    Specific-pathogen-free, female C.B-17 SCID mice

  • Dosages

    20 mg/kg

  • Administration

    i.v.

Selleck's 10074-G5 has been cited by 10 publications

SLC39A10 promotes malignant phenotypes of gastric cancer cells by activating the CK2-mediated MAPK/ERK and PI3K/AKT pathways [ Exp Mol Med, 2023, 10.1038/s12276-023-01062-5] PubMed: 37524874
Inhibiting the glycerophosphodiesterase EDI3 in ER-HER2+ breast cancer cells resistant to HER2-targeted therapy reduces viability and tumour growth [ J Exp Clin Cancer Res, 2023, 42(1):25] PubMed: 36670508
The calcium channel TRPC6 promotes chemotherapy-induced persistence by regulating integrin α6 mRNA splicing [ Cell Rep, 2023, 10.1016/j.celrep.2023.113347] PubMed: 37910503
The ABL-MYC axis controls WIPI1-enhanced autophagy in lifespan extension [ Commun Biol, 2023, 6(1):872] PubMed: 37620393
The ABL-MYC axis controls WIPI1-enhanced autophagy in lifespan extension [ Commun Biol, 2023, 6(1):872] PubMed: 37620393
The ABL-MYC axis controls WIPI1-enhanced autophagy in lifespan extension [ Commun Biol, 2023, 6(1):872] PubMed: 37620393
c-MYC-mediated TRIB3/P62+ aggresomes accumulation triggers paraptosis upon the combination of everolimus and ginsenoside Rh2 [ Acta Pharm Sin B, 2022, 12(3):1240-1253] PubMed: 35530150
The insulin and IGF signaling pathway sustains breast cancer stem cells by IRS2/PI3K-mediated regulation of MYC [ Cell Rep, 2022, 41(10):111759] PubMed: 36476848
c-Myc-PD-L1 Axis Sustained Gemcitabine-Resistance in Pancreatic Cancer [ Front Pharmacol, 2022, 13:851512] PubMed: 35586061
c-Myc Represses Transcription of Epstein-Barr Virus Latent Membrane Protein 1 Early after Primary B Cell Infection. [ J Virol, 2018, 92(2)] PubMed: 29118124

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.