| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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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. 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.
| Targets |
Daudi cells (IC50 = 15.6 μM); HL-60 cells (IC50 = 13.5 μM); c-Myc–Max (IC50 = 146 μM)
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| ln Vitro |
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| ln Vivo |
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| 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.
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| 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].
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| Animal Protocol |
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| References |
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| Molecular Formula |
C18H12N4O3
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| Molecular Weight |
332.31
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| Exact Mass |
332.09
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| Elemental Analysis |
C, 64.67; H, 4.22; N, 16.76; O, 14.36
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| CAS # |
413611-93-5
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| Related CAS # |
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| PubChem CID |
2836600
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| Appearance |
Pink to red solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
538.6±60.0 °C at 760 mmHg
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| Flash Point |
279.5±32.9 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.719
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| LogP |
4.97
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
25
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| Complexity |
466
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=[N+]([O-])C1=CC=C(NC2=CC=CC=C2C3=CC=CC=C3)C4=NON=C41
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| InChi Key |
KMJPYSQOCBYMCF-UHFFFAOYSA-N
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| 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
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| Chemical Name |
4-nitro-N-(2-phenylphenyl)-2,1,3-benzoxadiazol-7-amine
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.52 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| 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.
Calculation results
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.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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