10074-G5
Based on 2 publication(s) in Google Scholar
10074-G5 is an inhibitor of c-Myc-Max dimerization with an IC50 of 146 μM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.63%
- CAS. Nr.: 413611-93-5
- Formel: C18H12N4O3
- Molecular Weight:332.31
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) 10074-G5
More
Biologische Aktivität
IC50: 15.6 μM (Daudi cells), 13.5 μM (HL-60 cells)[1], 146 μM (c-Myc–Max)[2]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Daudi | EC50 |
10 μM
Compound: 10074-G5
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Antiproliferative activity against human Daudi assessed as inhibition of cell proliferation by MTT assay
Antiproliferative activity against human Daudi assessed as inhibition of cell proliferation by MTT assay
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[PMID: 33569941] |
| Daudi | IC50 |
10 μM
Compound: 1, 10074-G5
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Cytotoxicity against human Daudi cells assessed as growth inhibition after 3 to 5 days by MTT assay
Cytotoxicity against human Daudi cells assessed as growth inhibition after 3 to 5 days by MTT assay
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[PMID: 23177256] |
| HL-60 | EC50 |
30 μM
Compound: 10074-G5
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Antiproliferative activity against (unknown origin) HL-60 assessed as inhibition of cell proliferation by MTT assay
Antiproliferative activity against (unknown origin) HL-60 assessed as inhibition of cell proliferation by MTT assay
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[PMID: 33569941] |
| HL-60 | IC50 |
23 μM
Compound: 10074-G5
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Cytotoxicity against human HL-60 cells measured after 72 hrs by MTT assay
Cytotoxicity against human HL-60 cells measured after 72 hrs by MTT assay
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[PMID: 33460833] |
| HL-60 | IC50 |
23 μM
Compound: 10074-G5
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Inhibition of cell growth in human HL-60 cells incubated for 3 to 4 days by MTT assay
Inhibition of cell growth in human HL-60 cells incubated for 3 to 4 days by MTT assay
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[PMID: 38340508] |
| HL-60 | IC50 |
30 μM
Compound: 1, 10074-G5
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Cytotoxicity against human HL60 cells assessed as growth inhibition after 3 to 5 days by MTT assay
Cytotoxicity against human HL60 cells assessed as growth inhibition after 3 to 5 days by MTT assay
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[PMID: 23177256] |
| HL-60 | IC50 |
7.2 μM
Compound: 10074-G5
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Inhibition of cell development in human HL-60 cells
Inhibition of cell development in human HL-60 cells
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[PMID: 38340508] |
| LNCaP | IC50 |
8.7 μM
Compound: 10074-G5
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Cytotoxicity against human LNCAP cells assessed as reduction in cell viability after 96 hrs by prestoblue assay
Cytotoxicity against human LNCAP cells assessed as reduction in cell viability after 96 hrs by prestoblue assay
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[PMID: 30326371] |
10074-G5 inhibits the growth of Daudi Burkitt's lymphoma cells and disruptes c-Myc/Max dimerization. The IC50 values against Daudi and HL-60 cells are 15.6 and 13.5 μM, respectively[1]. 10074-G5 binds the Myc peptide Myc353-437 with a Kd value of 2.8 μM in the region Arg363-Ile381. 10074-G5 binds in a cavity that is created by a kink (Asp379-Ile381) in the N-terminus of an induced helical domain (Leu370–Arg378)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 413611-93-5
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Appearance Solid
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Molecular Weight 332.31
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Formel C18H12N4O3
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Color Pink to red
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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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell Commun Signal
Novel dual-targeting c-Myc inhibitor D347-2761 represses myeloma growth via blocking c-Myc/Max heterodimerization and disturbing its stability. [Abstract]2022 May 26;20(1):73. PMID: 35619182 -
Biomed Pharmacother
Synergistic combination of isogarcinol isolated from edible fruits of Garcinia multiflora and dexamethasone to overcome leukemia glucocorticoid resistance. [Abstract]2024 Jan:170:115936. PMID: 38039755
Lösungsmittel & Löslichkeit
DMSO : ≥ 28 mg/mL (84.26 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.52 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
10074-G5 is dissolved in DMSO and diluted with culture medium. Daudi cells or HL-60 cells in logarithmic growth are treated with 10074-G5 (1-100 μM). After 72 h, 50 μL of 1 mg/mL MTT is added to each well and incubated for 4 h. At the end of the incubation, medium containing drug and MTT is removed from each well, and 100 μl of DMSO is added, followed by shaking for 5 min. The absorbance at 570 nm is read[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: C.B-17 SCID mice bearing Daudi xenografts are stratified into the following groups (10 mice/group): control; vehicle control (0.01 ml/g body weight, once daily for 5 days); positive control, doxorubicin (2.5 mg/kg/dose, one dose every 4 days for three doses); and 10074-G5 (20 mg/kg/dose, once daily for 5 days). Mice are dosed intravenously on the appropriate schedule, and body weights and tumor volumes are recorded twice weekly[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (279 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Clausen DM, et al. 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. [Content Brief]
[2]. Chauhan J, et al. 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. [Content Brief]
[3]. Yap JL, et al. Pharmacophore identification of c-Myc inhibitor 10074-G5. Bioorg Med Chem Lett. 2013 Jan 1;23(1):370-4. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0092 mL | 15.0462 mL | 30.0924 mL | 75.2310 mL |
| 5 mM | 0.6018 mL | 3.0092 mL | 6.0185 mL | 15.0462 mL | |
| 10 mM | 0.3009 mL | 1.5046 mL | 3.0092 mL | 7.5231 mL | |
| 15 mM | 0.2006 mL | 1.0031 mL | 2.0062 mL | 5.0154 mL | |
| 20 mM | 0.1505 mL | 0.7523 mL | 1.5046 mL | 3.7615 mL | |
| 25 mM | 0.1204 mL | 0.6018 mL | 1.2037 mL | 3.0092 mL | |
| 30 mM | 0.1003 mL | 0.5015 mL | 1.0031 mL | 2.5077 mL | |
| 40 mM | 0.0752 mL | 0.3762 mL | 0.7523 mL | 1.8808 mL | |
| 50 mM | 0.0602 mL | 0.3009 mL | 0.6018 mL | 1.5046 mL | |
| 60 mM | 0.0502 mL | 0.2508 mL | 0.5015 mL | 1.2538 mL | |
| 80 mM | 0.0376 mL | 0.1881 mL | 0.3762 mL | 0.9404 mL |
10074-G5 Related Classifications
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