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10074-G5

Name: 10074-G5
Brand: TargetMol
SKU: T3686
Price: 35 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T3686Cas No. 413611-93-5

10074-G5 is an inhibitor of c-Myc-Max dimerization.

10074-G5

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Purity: 99.94%

Catalog No. T3686Cas No. 413611-93-5

10074-G5 is an inhibitor of c-Myc-Max dimerization.

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$35	In Stock	In Stock
5 mg	$57	In Stock	In Stock
10 mg	$80	In Stock	In Stock
25 mg	$145	In Stock	In Stock
50 mg	$237	In Stock	In Stock
100 mg	$417	In Stock	In Stock
200 mg	$595	In Stock	In Stock
500 mg	$948	-	In Stock
1 mL x 10 mM (in DMSO)	$63	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Batch Information

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Purity:99.94%

Appearance:Solid

Color:Orange to Red

Resource Download

COA HNMR LCMS

Product Introduction

Bioactivity

Description	10074-G5 is an inhibitor of c-Myc-Max dimerization.
Targets&IC50	c-Myc: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, 10074-G5 inhibits the growth of Daudi Burkitt's lymphoma cells and disrupts c-Myc/Max dimerization. Daudi cells accumulates 10074-G5, and the highest intracellular concentration is observed at 6 h. 10074-G5 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 10074-G5, c-Myc protein expression decreases approximately 40% compared with vehicle-treated control. 10074-G5 is cytotoxic in vitro against Daudi and HL-60 cells, which overexpress c-Myc [2].
In vivo	The plasma half-life of 10074-G5 in mice treated with 20 mg/kg i.v. is 37 minutes, with a peak plasma concentration of 58 μM, 10-fold higher than peak tumor concentration. The rapid metabolism of 10074-G5 to inactive metabolites likely causes insufficient tumor concentrations to inhibit c-Myc/Max dimerization. A plasma peak concentration (Cmax) of 58.5 ± 2.7 nmol/ml is observed at 5 minutes post-intravenous administration in mice bearing Daudi xenografts, with plasma concentrations declining rapidly. Except for lung, liver, and fat, tissue concentrations are lower than plasma at all time points[2].
Cell Research	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 12,000 g 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.(Only for Reference)

Chemical Properties

Molecular Weight	332.31
Formula	C₁₈H₁₂N₄O₃
Cas No.	413611-93-5
Smiles	[O-][N+](=O)c1ccc(Nc2ccccc2-c2ccccc2)c2nonc12
Relative Density.	1.408 g/cm3 (Predicted)

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 55 mg/mL (165.51 mM), Sonication is recommended.

Ethanol: 10 mg/mL (30.09 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.02 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	3.0092 mL	15.0462 mL	30.0924 mL	150.4619 mL
5 mM	0.6018 mL	3.0092 mL	6.0185 mL	30.0924 mL
10 mM	0.3009 mL	1.5046 mL	3.0092 mL	15.0462 mL
20 mM	0.1505 mL	0.7523 mL	1.5046 mL	7.5231 mL

DMSO

	1mg	5mg	10mg	50mg
50 mM	0.0602 mL	0.3009 mL	0.6018 mL	3.0092 mL
100 mM	0.0301 mL	0.1505 mL	0.3009 mL	1.5046 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc