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Birabresib

Name: Birabresib
Brand: TargetMol
SKU: T6032
Price: 41 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T6032Cas No. 202590-98-5

Alias OTX015 (MK 8628/Birabresib), OTX-015, MK-8628

Birabresib (MK-8628) is a synthetic, small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins 2, 3 and 4 with potential antineoplastic activity.

Birabresib

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Purity: 99.36%

Catalog No. T6032Alias OTX015 (MK 8628/Birabresib), OTX-015, MK-8628Cas No. 202590-98-5

Birabresib (MK-8628) is a synthetic, small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins 2, 3 and 4 with potential antineoplastic activity.

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$41	In Stock	In Stock
5 mg	$67	In Stock	In Stock
10 mg	$87	In Stock	In Stock
25 mg	$153	In Stock	In Stock
50 mg	$247	In Stock	In Stock
100 mg	$417	In Stock	In Stock
200 mg	$622	In Stock	In Stock
500 mg	$992	-	In Stock
1 mL x 10 mM (in DMSO)	$72	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:99.36%

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Birabresib (MK-8628) is a synthetic, small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins 2, 3 and 4 with potential antineoplastic activity.
Targets&IC50	BRDs:10-19 nM(EC50)
In vitro	Birabresib inhibits the binding of BRD2, BRD3, and BRD4 to AcH4 with IC50 ranging from 92 to 112 nM, and inhibits the growth of a variety of human cancer cell lines with GI50 ranging from 60 to 200 nM. [1] Birabresib results in rapid down-regulation of c-MYC expression, and show the synergistic anti-proliferative effects in combination with ALK inhibitors in ALKpos ALCL cell lines. [2]
In vivo	OTX015 (p.o.) significantly inhibits the growth of Ty82 BRD-NUT midline carcinoma tumors in nude mice by 79% at 100 mg/kg qd and 61% at 10 mg/kg bid, respectively. [1]
Kinase Assay	TR-FRET Assay [1]: To assess binding of OTX015 to BRD2, BRD3, and BRD4, BRD-expressing CHO cell lysate (from CHO cells transfected with expression plasmids for Flag-tagged BRD2, BRD3, or BRD4 or vector alone), europium-conjugated anti-Flag antibody, XL-665-conjugated streptavidin, and biotinylated OTX015 are incubated at room temperature for 0.2 to 2 h. Fluorescence is measured by TR-FRET using an EnVision 2103 Multilabel Reader and EC50 for binding is calculated by nonlinear regression using PRISM version 5.02.
Cell Research	Effects of OTX015 on cancer cell proliferation are evaluated by incubating human tumor cells for 72 h with increasing concentrations of OTX015 and assessing proliferation using a tetrazolium salt (WST-8)-based colorimetric assay.(Only for Reference)
Synonyms	OTX015 (MK 8628/Birabresib), OTX-015, MK-8628

Chemical Properties

Molecular Weight	491.99
Formula	C₂₅H₂₂ClN₅O₂S
Cas No.	202590-98-5
Smiles	CC=1C2=C(N3C([C@H](CC(NC4=CC=C(O)C=C4)=O)N=C2C5=CC=C(Cl)C=C5)=NN=C3C)SC1C
Relative Density.	1.45 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

Ethanol: 9.8 mg/mL (19.92 mM), Sonication is recommended.

DMSO: 255 mg/mL (518.3 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.07 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	2.0326 mL	10.1628 mL	20.3256 mL	101.6281 mL
5 mM	0.4065 mL	2.0326 mL	4.0651 mL	20.3256 mL
10 mM	0.2033 mL	1.0163 mL	2.0326 mL	10.1628 mL

DMSO

	1mg	5mg	10mg	50mg
20 mM	0.1016 mL	0.5081 mL	1.0163 mL	5.0814 mL
50 mM	0.0407 mL	0.2033 mL	0.4065 mL	2.0326 mL
100 mM	0.0203 mL	0.1016 mL	0.2033 mL	1.0163 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