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10074-G5

Cat. No. M2353
10074-G5 Structure
Size Price Availability Quantity
5mg USD 75  USD75 In stock
10mg USD 105  USD105 In stock
25mg USD 175  USD175 In stock
50mg USD 285  USD285 In stock
100mg USD 500  USD500 In stock
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Quality Control & Documentation
Biological Activity

10074-G5 is an inhibitor of c-Myc-Max dimerization (IC50 =146 μM) that operates by binding and stabilizing c-Myc in its monomeric form. 10074-G5 inhibits c-Myc/Max heterodimer formation and its transcriptional activity. 10074-G5 is most efficient in inducing neuronal differentiation and lipid accumulation in MYCN-amplified neuroblastoma cells.

Product Citations
Chemical Information
Molecular Weight 332.31
Formula C18H12N4O3
CAS Number 413611-93-5
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Chauhan J, et al. ChemMedChem. Discovery of Methyl 4'-Methyl-5-(7-nitrobenzo[c][1,2,5]oxadiazol-4-yl)-[1,1'-biphenyl]-3-carboxylate, an Improved Small-Molecule Inhibitor of c-Myc-Max Dimerization.

[2] Müller I, et al. PloS one. Targeting of the MYCN Protein with Small Molecule c-MYC Inhibitors.

[3] Clausen DM, et al. Journal of Pharmacology and Experimental Therapeutics. In vitro cytotoxicity and in vivo efficacy, pharmacokinetics, and metabolism of 10074-G5, a novel small-molecule inhibitor of c-Myc/Max dimerization.

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Keywords: 10074-G5 supplier, c-Myc, inhibitors, activators


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