10074-G5

Alias: 10074-G5; 10074G5; 10074 G5
Cat No.:V2724 Purity: ≥98%
10074-G5 is a potent inhibitor of c-Myc-Max dimerization and interaction with an IC50 of 146 μM and with anticancer activities.
10074-G5 Chemical Structure CAS No.: 413611-93-5
Product category: c-Myc
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

10074-G5 is a potent inhibitor of c-Myc-Max dimerization and interaction with an IC50 of 146 μM and with anticancer activities. The binding and distortion of the bHLH-ZIP domain of c-Myc by 10074-G5 results in the inhibition of both the transcriptional activity and the formation of the c-Myc/Max heterodimer. 10074-G5 hampered c-Myc/Max dimerization and delayed the growth of Daudi Burkitt's lymphoma cells in vitro. The C.B-17 SCID mice treated with 20 mg/kg 10074-G5 intravenously for 5 days in a row showed no growth inhibition of Daudi xenografts after the treatment. Neither two nor twenty-four hours following treatment showed any inhibition of c-Myc/Max dimerization in Daudi xenografts.

Biological Activity I Assay Protocols (From Reference)
Targets
Daudi cells (IC50 = 15.6 μM); HL-60 cells (IC50 = 13.5 μM); c-Myc–Max (IC50 = 146 μM)
ln Vitro

10074-G5 prevents c-Myc/Max dimerization and suppresses the growth of Daudi Burkitt's lymphoma cells. Regarding Daudi and HL-60 cells, the IC50 values are 15.6 and 13.5 μM, correspondingly[1]. Myc peptide Myc353-437 is bound by 10074-G5 in the Arg363-Ile381 region at a Kd value of 2.8 μM. Upon kinking (Asp379-Ile381) in the N-terminus of an induced helical domain (Leu370–Arg378), 10074-G5 binds in a cavity formed.[3].

ln Vivo
In mice given 20 mg/kg i.v. of 10074-G5, the plasma half-life is 37 min, and the peak plasma concentration was 58 μM, ten times higher than the peak tumor concentration[1].
Enzyme Assay
With a 146 μM IC50 and anticancer properties, 10074-G5 is a strong inhibitor of c-Myc-Max dimerization and interaction. By binding to and altering the bHLH-ZIP domain of c-Myc, 10074-G5 prevents the formation of the c-Myc/Max heterodimer and its transcriptional activity.
Cell Assay
After dissolving in DMSO, 10074-G5 is diluted with culture medium. In logarithmic growth, Daudi cells or HL-60 cells are exposed to 10074-G5 (1-100 μM). Each well receives 50 μL of 1 mg/mL MTT after 72 hours, and it is then incubated for 4 hours. Upon completion of the incubation period, the drug-containing medium and MTT are extracted from each well, and 100 μl of DMSO is added. A 5-minute shaking period is then observed. It reads the absorbance at 570 nm[1].
Animal Protocol
Mice: The following groups of 10 C.B-17 SCID mice carrying Daudi xenografts are arranged as follows: control; positive control, doxorubicin (2.5 mg/kg/dose, one dose every 4 days for three doses); 10074-G5 (20 mg/kg/dose, once daily for five days); and vehicle control (0.01 ml/g body weight, once daily for five days). Two times a week, body weights and tumor volumes are measured in mice given intravenous doses according to the prescribed schedule[1].
References

[1]. In vitro cytotoxicity and in vivo efficacy, pharmacokinetics, and metabolism of 10074-G5, a novel small-molecule inhibitor of c-Myc/Max dimerization. J Pharmacol Exp Ther. 2010 Dec;335(3):715-27.

[2]. 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. ChemMedChem. 2014 Oct;9(10):2274-85.

[3]. Pharmacophore identification of c-Myc inhibitor 10074-G5. Bioorg Med Chem Lett. 2013 Jan 1;23(1):370-4.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C18H12N4O3
Molecular Weight
332.31
Exact Mass
334.34
Elemental Analysis
C, 64.67; H, 4.22; N, 16.76; O, 14.36
CAS #
413611-93-5
Appearance
Solid powder
SMILES
C1=CC=C(C=C1)C2=CC=CC=C2NC3=CC=C(C4=NON=C34)[N+](=O)[O-]
InChi Key
KMJPYSQOCBYMCF-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H12N4O3/c23-22(24)16-11-10-15(17-18(16)21-25-20-17)19-14-9-5-4-8-13(14)12-6-2-1-3-7-12/h1-11,19H
Chemical Name
4-nitro-N-(2-phenylphenyl)-2,1,3-benzoxadiazol-7-amine
Synonyms
10074-G5; 10074G5; 10074 G5
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~60 mg/mL (~180.5 mM)
Water: <1 mg/mL
Ethanol: ~10 mg/mL (~30.0 mM)
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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Biological Data
  • 10074-G5

    In vitro analysis of 10074-G5 against Daudi Burkitts lymphoma cells.J Pharmacol Exp Ther.2010 Dec;335(3):715-27.
  • 10074-G5

    Efficacy study of 10074-G5 in mice bearing Daudi tumor xenografts.J Pharmacol Exp Ther.2010 Dec;335(3):715-27.
  • 10074-G5

    Coimmunoprecipitation and immunoblot analysis of c-Myc and Max protein expression in Daudi xenografts from mice treated for 5 days with 20 mg/kg i.v. 10074-G5.J Pharmacol Exp Ther.2010 Dec;335(3):715-27.
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