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Birabresib

Catalog No. T6032 CAS 202590-98-5

Synonyms: OTX-015, OTX015 （MK 8628/Birabresib）, 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.

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Birabresib, CAS 202590-98-5

Pack Size	Availability	Price/USD
2 mg	In stock	$ 41.00
5 mg	In stock	$ 67.00
10 mg	In stock	$ 87.00
25 mg	In stock	$ 153.00
50 mg	In stock	$ 247.00
100 mg	In stock	$ 417.00
200 mg	In stock	$ 622.00
500 mg	In stock	$ 992.00
1 mL * 10 mM (in DMSO)	In stock	$ 72.00

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Purity: 99.93%

Purity: 99.09%

Purity: 99.06%

Biological Description

Chemical Properties

Storage & Solubility Information

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	OTX015 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] OTX015 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 <a href="#s_ref" class="sref">[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	OTX-015, OTX015 （MK 8628/Birabresib）, MK-8628
Molecular Weight	491.99
Formula	C25H22ClN5O2S
CAS No.	202590-98-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 9.8 mg/mL (20 mM)

DMSO: 49.2 mg/mL (100 mM)

References and Literature

1. Noel JK, et al. Mol Cancer Ther. 2013, 12, C244. 2. Boi M, et al. Mol Cancer Ther. 2013, 12, A219.

Citations

1. Zhang G M, Huang S S, Ye L X, et al. Reciprocal positive regulation between BRD4 and YAP in GNAQ-mutant uveal melanoma cells confers sensitivity to BET inhibitors. Pharmacological Research. 2022: 106464.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Anti-Cancer Compound Library Preclinical Compound Library Clinical Compound Library Anti-Aging Compound Library NO PAINS Compound Library

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PROTAC BRD4 Degrader-2 Histone Acetyltransferase Inhibitor II JQ-1 (carboxylic acid) ZEN-3411 ARV-771 EML 425 MS31 trihydrochloride (2366264-12-0 free base) XMD8-92

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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.

Keywords

Birabresib 202590-98-5 Chromatin/Epigenetic Epigenetic Reader Domain OTX 015 Inhibitor OTX-015 OTX015 MK8628 MK 8628 MK 8628/Birabresib OTX015 （MK 8628/Birabresib） inhibit MK-8628 inhibitor

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