In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml
Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO
40%PEG300
5%Tween80
50%ddH2O
Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.
0.330mg/ml
(0.99mM)
Taking the 1 mL working solution as an example, add 50 μL of 6.6 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution
5% DMSO
95% Corn oil
Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.
0.150mg/ml
(0.45mM)
Taking the 1 mL working solution as an example, add 50 μL of 3 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
* <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.)
Preparing Stock Solutions
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 (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, this compound inhibits the growth of Daudi Burkitt's lymphoma cells and disrupts c-Myc/Max dimerization. Daudi cells accumulate this chemical, and the highest intracellular concentration is observed at 6 h. It 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 of this compound, c-Myc protein expression decreases approximately 40% compared with vehicle-treated control. It 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 tumour concentration. The lack of antitumour activity probably is caused by the rapid metabolism of this compound to inactive metabolites, resulting in tumour concentrations of this chemical insufficient to inhibit c-Myc/Max dimerization. Plasma 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, its concentration in plasma declines rapidly. Except for lung, liver, and fat, tissue concentrations of this compound are lower than those of plasma at all time points.
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.
Sellecks 10074-G5 Has Been Cited by 11 Publications
Genome-wide CRISPR screening identifies PHF8 as an effective therapeutic target for KRAS- or BRAF-mutant colorectal cancers
[ J Exp Clin Cancer Res, 2025, 44(1):70]
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]
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]
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]
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
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.
