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SGC0946

Name: SGC0946
Brand: TargetMol
SKU: T3082
Price: 37 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T3082Cas No. 1561178-17-3

SGC0946 is a highly effective and specific DOT1L methyltransferase inhibitor (IC50: 0.3 nM); selectively kill mixed lineage leukemia cells.

SGC0946

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Purity: 99.82%

Catalog No. T3082Cas No. 1561178-17-3

SGC0946 is a highly effective and specific DOT1L methyltransferase inhibitor (IC50: 0.3 nM); selectively kill mixed lineage leukemia cells.

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$37	In Stock	In Stock
5 mg	$57	In Stock	In Stock
10 mg	$98	In Stock	In Stock
25 mg	$183	In Stock	In Stock
50 mg	$263	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$77	In Stock	In Stock

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

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.82%

Appearance:Solid

Color:White

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Product Introduction

Bioactivity

Description	SGC0946 is a highly effective and specific DOT1L methyltransferase inhibitor (IC50: 0.3 nM); selectively kill mixed lineage leukemia cells.
Targets&IC50	DOT1L:0.3 nM
In vivo	SGC 0946 significantly decreases di-methylation of H3K79 in A431 cells (IC50: 2.6 nM) and MCF10A cells (IC50: 8.8 nM), effectively and selectively killing cells with MLL translocations. Compared to its analogue EPZ004777, SGC 0946 is more potent against DOT1L, making it promising for cancer research. Moreover, SGC 0946 demonstrates over 100-fold higher selectivity for DOT1L than other histone methyltransferases (HMTs).
Kinase Assay	Determination of Inhibitor IC50 Values: EPZ004777 is serially diluted 3-fold in DMSO for a total of ten concentrations, beginning at 1 mM. A 1 μL aliquot of each inhibitor dilution is plated in a 384-well microtiter plate. The 100% inhibition control consisted of 2.5 mM ?nal concentration of the product inhibitor S-adenosyl-L-homocysteine, (SAH). Compound is incubated for 30 min with 40 ml per well of 0.25 nM DOT1L(1-416) in assay buffer (20 mM TRIS [pH 8.0] 10 mM NaCl, 0.002% Tween 20, 0.005% Bovine Skin Gelatin, 100 mM KCl, and 0.5 mM DTT). 10 ml per well of substrate mix comprising assay buffer with 200 nM 3H-SAM (American Radiolabeled Chemicals: 80 Ci/mmol), 600 nM unlabeled SAM, and 20 nM nucleosomes are added to initiate the reaction (both substrates are present in the ?nal reaction mixture at their respective KM values). Reactions are incubated for 120 min and quenched with 10 ml per well of 800 mM SAM. Incorporation of radioactivity into nucleosome substrate is measured in a ?ashplate. IC50 values for enzymes in the histone methyltransferase panel are determined under similar balanced assay conditions with both SAM and protein/peptide substrate present at concentrations equal to their respective KM values.

Chemical Properties

Molecular Weight	618.57
Formula	C₂₈H₄₀BrN₇O₄
Cas No.	1561178-17-3
Smiles	CC(C)N(CCCNC(=O)Nc1ccc(cc1)C(C)(C)C)C[C@H]1O[C@H]([C@H](O)[C@@H]1O)n1cc(Br)c2c(N)ncnc12
Relative Density.	1.48 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature | 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: 150 mg/mL (242.49 mM), Sonication is recommended.

Ethanol: 93 mg/mL (150.35 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (5.33 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	1.6166 mL	8.0832 mL	16.1663 mL	80.8316 mL
5 mM	0.3233 mL	1.6166 mL	3.2333 mL	16.1663 mL
10 mM	0.1617 mL	0.8083 mL	1.6166 mL	8.0832 mL
20 mM	0.0808 mL	0.4042 mL	0.8083 mL	4.0416 mL
50 mM	0.0323 mL	0.1617 mL	0.3233 mL	1.6166 mL
100 mM	0.0162 mL	0.0808 mL	0.1617 mL	0.8083 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