10074-G5

Name: 10074-G5
Brand: MedChemExpress
SKU: HY-100996
Rating: 5.0 (2 reviews)

製品番号: HY-100996 純度: 99.63%: Data Sheet SDS COA 取扱説明書
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10074-G5 is an inhibitor of c-Myc-Max dimerization with an IC₅₀ of 146 μM.

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10074-G5 構造式

CAS 番号 : 413611-93-5

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 79	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 79	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$72	在庫あり	Estimated Time of Arrival: December 31
10 mg	$102	在庫あり	Estimated Time of Arrival: December 31
25 mg	$180	在庫あり	Estimated Time of Arrival: December 31
50 mg	$288	在庫あり	Estimated Time of Arrival: December 31
100 mg	$504	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

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Based on 2 publication(s) in Google Scholar

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10074-G5 (Standard) お問い合わせ

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製品説明

10074-G5 is an inhibitor of c-Myc-Max dimerization with an IC₅₀ of 146 μM.

IC₅₀ & Target

IC50: 15.6 μM (Daudi cells), 13.5 μM (HL-60 cells)^[1], 146 μM (c-Myc–Max)^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
Daudi	EC₅₀	10 μM Compound: 10074-G5	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	[PMID: 33569941]
Daudi	IC₅₀	10 μM Compound: 1, 10074-G5	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	[PMID: 23177256]
HL-60	EC₅₀	30 μM Compound: 10074-G5	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	[PMID: 33569941]
HL-60	IC₅₀	23 μM Compound: 10074-G5	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	[PMID: 33460833]
HL-60	IC₅₀	23 μM Compound: 10074-G5	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	[PMID: 38340508]
HL-60	IC₅₀	30 μM Compound: 1, 10074-G5	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	[PMID: 23177256]
HL-60	IC₅₀	7.2 μM Compound: 10074-G5	Inhibition of cell development in human HL-60 cells Inhibition of cell development in human HL-60 cells	[PMID: 38340508]
LNCaP	IC₅₀	8.7 μM Compound: 10074-G5	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	[PMID: 30326371]

体外実験

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 K_d 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.

体内実験

The plasma half-life of 10074-G5 in mice treated with 20 mg/kg i.v. is 37 min, and peak plasma concentration was 58 μM, which is 10-fold higher than peak tumor concentration^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

332.31

分子式

C₁₈H₁₂N₄O₃

CAS 番号

413611-93-5

Appearance

Solid

Color

Pink to red

SMILES

O=[N+]([O-])C1=CC=C(NC2=CC=CC=C2C3=CC=CC=C3)C4=NON=C41

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

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.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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.

Protocol 1

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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

純度とドキュメンテーション

純度: 99.63%

Select Batch:

データシート (279 KB) SDS (480 KB)

COA (253 KB) HNMR (253 KB) LCMS (96 KB)

取扱説明書 (2659 KB)

参考文献

[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]

細胞実験 ^[1]	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) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[1]	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) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[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

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

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

10074-G5413611-93-5c-MycAutophagyMycInhibitorinhibitorinhibit

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10074-G5

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Other Forms of 10074-G5:

10074-G5 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

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参考文献

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10074-G5 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

10074-G5 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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