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BETd-246

Name: BETd-246
Brand: TargetMol
SKU: T14549
Rating: 4.5 (1 reviews)

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Catalog No. T14549Cas No. 2140289-17-2

BETd-246 is an inhibitor of second-generation and PROTAC-based BET bromodomain (BRD), show antitumor activity.

BETd-246

😃Good

Catalog No. T14549Cas No. 2140289-17-2

BETd-246 is an inhibitor of second-generation and PROTAC-based BET bromodomain (BRD), show antitumor activity.

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$539	Inquiry	Inquiry
10 mg	$789	Inquiry	Inquiry
25 mg	$1,610	Inquiry	Inquiry
50 mg	$2,440	Inquiry	Inquiry
100 mg	Inquiry	Inquiry	Inquiry
200 mg	Inquiry	Inquiry	Inquiry

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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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Product Introduction

Bioactivity

Description	BETd-246 is an inhibitor of second-generation and PROTAC-based BET bromodomain (BRD), show antitumor activity.
In vitro	BETd-246 treatment (0-100 nM, 1-3 h) leads to a dose-dependent reduction of BRD2, BRD3, and BRD4 in TNBC cell lines, with optimal effects observed at 30-100 nM for 1 hour or 10-30 nM for 3 hours. BETd-246 (100 nM, 24/48 hours) significantly inhibits growth and induces apoptosis in MDA-MB-468 cell lines. Additionally, BETd-246 (100 nM, 24 hours) causes marked cell cycle arrest and apoptosis in TNBC cell lines[1]. It induces rapid, time-dependent downregulation of MCL1 protein in all evaluated TNBC cell lines and exhibits stronger apoptosis induction than BETi-211.
In vivo	BETd-246 (5 mg/kg, IV, 3 times per week for 3 weeks) effectively inhibits WHIM24 tumor growth, similar to the antitumor activity of BETi-211 at a higher dose with more frequent administration. BETd-246 exhibits limited drug exposure in xenograft tumor tissue in MDA-M-231 and MDA-MB-468 models[1]. A dose of 10 mg/kg induces partial tumor regression during treatment without apparent toxicity.

Chemical Properties

Molecular Weight	946.02
Formula	C₄₈H₅₅N₁₁O₁₀
Cas No.	2140289-17-2
Smiles	O=C(NCCCOCCOCCOCCCNC1=CC=CC=2C(=O)N(C(=O)C12)C3C(=O)NC(=O)CC3)C4=NC=5NC=6C=C(C(OC)=CC6C5C(=N4)NC7=CC(=NN7CC)C8CC8)C=9C(=NOC9C)C
Relative Density.	1.51 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 200 mg/mL (211.41 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 5 mg/mL (5.29 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	1.0571 mL	5.2853 mL	10.5706 mL	52.8530 mL
5 mM	0.2114 mL	1.0571 mL	2.1141 mL	10.5706 mL
10 mM	0.1057 mL	0.5285 mL	1.0571 mL	5.2853 mL
20 mM	0.0529 mL	0.2643 mL	0.5285 mL	2.6427 mL
50 mM	0.0211 mL	0.1057 mL	0.2114 mL	1.0571 mL
100 mM	0.0106 mL	0.0529 mL	0.1057 mL	0.5285 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