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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
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 recommeded.

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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

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