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dBET6

Name: dBET6
Brand: TargetMol
SKU: T5130
Price: 48 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T5130Cas No. 1950634-92-0

dBET6 is a selective and cell-permeable degrader of BET based on PROTAC (IC50: 14 nM). It has antitumor activity.

dBET6

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Purity: 99.12%

Catalog No. T5130Cas No. 1950634-92-0

dBET6 is a selective and cell-permeable degrader of BET based on PROTAC (IC50: 14 nM). It has antitumor activity.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$48	In Stock	In Stock
5 mg	$98	In Stock	In Stock
10 mg	$172	In Stock	In Stock
25 mg	$323	In Stock	In Stock
50 mg	$518	In Stock	In Stock
100 mg	$749	In Stock	In Stock
200 mg	$945	In Stock	In Stock
500 mg	$1,380	-	In Stock
1 mL x 10 mM (in DMSO)	$159	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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Batch Information

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Purity:99.12%

Appearance:Solid

Color:White

Resource Download

COA HPLC HNMR

Product Introduction

Bioactivity

Description	dBET6 is a selective and cell-permeable degrader of BET based on PROTAC (IC50: 14 nM). It has antitumor activity.
Targets&IC50	BET:14 nM
In vitro	dBET6 (100 nM) exhibits antitumor activity against T cell acute lymphoblastic leukemia (T-ALL) lines via degradation of BRD4.
In vivo	dBET6 (7.5 mg/kg, p.o., BID) reduces leukemic burden in a disseminated mouse model of T-ALL.
Animal Research	MOLT4 human T-ALL cells are intravenously injected into NSG mice (2×106 cells/mouse). Luminescence is utilized to monitor engraftment (evident at day 6), at which point mice are randomized into three cohorts that receive dBET6 (7.5 mg/kg BID, n = 8), JQ1 (20 mg/kg QD, n = 9) or vehicle (captisol, n = 9) treatment for 14 days. Survival of all three cohorts is subsequently monitored using hind limb paralysis caused by a high femoral leukemic burden as a defined endpoint. SUPT11 human T-ALL cells (mCherry+ and Luciferase+) are intravenously injected into NSG mice (2.52×106 cells/mouse). Luminescence is used to monitor successful engraftment, occurring 10 days after injection. At this point, animals are randomized into three cohorts that receive dBET6 (7.5 mg/kg BID, n = 7), JQ1 (7.5 mg/kg BID, n = 7) or vehicle (captisol, n = 7) treatment for 18 days. Treatment burden is assessed via total body luminescence imaging as well as by bone marrow infiltration by mCherry+ T-ALL cells.

Chemical Properties

Molecular Weight	841.37
Formula	C₄₂H₄₅ClN₈O₇S
Cas No.	1950634-92-0
Smiles	CC=1C2=C(N3C([C@H](CC(NCCCCCCCCNC(COC4=C5C(C(=O)N(C5=O)C6C(=O)NC(=O)CC6)=CC=C4)=O)=O)N=C2C7=CC=C(Cl)C=C7)=NN=C3C)SC1C
Relative Density.	1.48 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 112.5 mg/mL (133.71 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 1 mg/mL (1.19 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

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.1885 mL	5.9427 mL	11.8854 mL	59.4269 mL
5 mM	0.2377 mL	1.1885 mL	2.3771 mL	11.8854 mL
10 mM	0.1189 mL	0.5943 mL	1.1885 mL	5.9427 mL
20 mM	0.0594 mL	0.2971 mL	0.5943 mL	2.9713 mL
50 mM	0.0238 mL	0.1189 mL	0.2377 mL	1.1885 mL
100 mM	0.0119 mL	0.0594 mL	0.1189 mL	0.5943 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