Birabresib (OTX015)

Catalog No.S7360 Synonyms: MK 8628

For research use only.

Birabresib (OTX015, MK 8628) is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays. Birabresib inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.

Birabresib (OTX015) Chemical Structure

CAS No. 202590-98-5

Selleck's Birabresib (OTX015) has been cited by 56 publications

Purity & Quality Control

Choose Selective Epigenetic Reader Domain Inhibitors

Biological Activity

Description Birabresib (OTX015, MK 8628) is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays. Birabresib inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.
Features Orally bioavailable BRD2/3/4-selective inhibitor that has been tested in Phase I clinical trials for treatment of Haematological Malignancies.
Targets
BRDs [1]
(Cell-free assay)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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MV4-11 MVXGeY5kfGmxbjDhd5NigQ>? NWn0dYZ{OzFwMkWgeI8hOTJ3IH7N MoTCOkBpenN? MYrJcohq[mm2aX;uJI9nKEKURESgbY4hcHWvYX6gUXY1NTFzIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBETEt4IH3SUmEhdGW4ZXygZZQhOzFwMkWgeI8hOTJ3IH7NJI1m[XO3cnXkJIFnfGW{IE[gbJJ{KGK7IGPZRnIh\3KnZX6g[JlmKGKjc3XkJHJVNXGSQ2KgZY5idHm|aYO= NWjPVoFlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{KyNFg3ODBpPkOyNlA5PjByPD;hQi=>
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MV4-11 NUPQRmR5TnWwY4Tpc44h[XO|YYm= NELafHkyOCC2bzCxNFAhdk1? NETvOlMzPCCqcoO= NVfyZoVFUW6qaXLpeIlwdiCxZjDCVmQ1KGmwIHj1cYFvKE2YND2xNUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iYz3NfYMhdVKQQTDs[ZZmdCCjdDCxNEB1dyBzMECgcm0h[W[2ZYKgNlQhcHK|IHL5JJJm[WxidHnt[UByWEOUIHHuZYx6e2m| NVvre|dRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G0PVAxPzBpPkOxOFkxODdyPD;hQi=>
MV4-11 NUjVcYdOSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M1LRXVczKGi{cx?= MUXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2YND2xNUBk\WyuczDh[pRmeiB5MjDodpMh[nliQ1PLPEBweiCVUlKgZZN{[Xl? MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTR7MEC3NEc,OzF2OUCwO|A9N2F-
MV4-11 MmLjRZBweHSxc3nzJIF{e2G7 MXqyOEBpenN? MlrrTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCPVkStNVEh[2WubIOgZYZ1\XJiMkSgbJJ{KGK7IFHucoV5cW5iVjDzeIFqdmmwZzDiZZNm\CCjc4PhfS=> MkC0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF2OUCwO|AoRjNzNEmwNFcxRC:jPh?=
RKO MoHuR4VtdCCleXPs[UBie3OjeR?= NYrHbplOOTByIH7N MUWyOEBpenN? MoXPTY5lfWO2aX;uJI9nKGOnbHygZ5lkdGViYYLy[ZN1KGmwIHj1cYFvKFKNTzDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG|ZTDpckBi[2O3bYXsZZRqd25iYYSgS|EheGijc3WgZZQhOTByIH7NJIFnfGW{IEK0JIhzeyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pIHLhd4VlKG[ub4egZ5l1d22ndILpZ{BidmGueYPpdy=> MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTR7MEC3NEc,OzF2OUCwO|A9N2F-
Assay
Methods Test Index PMID
Western blot BRD4 ; c-Myc ; JAK2 / p-STAT5 / STAT5 / p-STAT3 / c-Myc / PIM1 / CDK6 / HEXIM1 / p27 / p21 / Bcl-xL / γH2AX ; ZO-1 / Vimentin 26051217 28042144 27980063
Immunofluorescence BRD4 ; Vimentin 28042144 27980063
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]

Protocol (from reference)

Kinase Assay:

[1]

  • 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:

[1]

  • Cell lines: Human tumor cells
  • Concentrations: ~2 μM
  • Incubation Time: 72 hours
  • Method:

    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.

Animal Research:

[1]

  • Animal Models: BLAB/c-nu/nu mice bearing established Ty82 BRD-NUT midline carcinoma xenografts.
  • Dosages: ~100 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

5mg/mL

Chemical Information

Molecular Weight 491.99
Formula

C25H22ClN5O2S

CAS No. 202590-98-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)NC4=CC=C(C=C4)O)C5=CC=C(C=C5)Cl)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02698176 Terminated Drug: Birabresib NUT Midline Carcinoma (NMC)|Triple Negative Breast Cancer (TNBC)|Non-small Cell Lung Cancer (NSCLC)|Castration-resistant Prostate Cancer (CRPC) Merck Sharp & Dohme LLC May 4 2016 Phase 1
NCT02698189 Terminated Drug: Birabresib Dose 20 mg AML Including AML de Novo and AML Secondary to MDS|DLBCL Merck Sharp & Dohme LLC May 19 2016 Phase 1
NCT02296476 Terminated Drug: Birabresib Glioblastoma Multiforme Oncoethix GmbH October 29 2014 Phase 2
NCT02259114 Completed Drug: Birabresib NUT Midline Carcinoma|Triple Negative Breast Cancer|Non-small Cell Lung Cancer With Rearranged ALK Gene/Fusion Protein or KRAS Mutation|Castrate-resistant Prostate Cancer|CRPC|Pancreatic Ductal Adenocarcinoma Oncoethix GmbH October 23 2014 Phase 1
NCT01713582 Completed Drug: OTX015/Birabresib Acute Myeloid Leukemia|Diffuse Large B-cell Lymphoma|Acute Lymphoblastic Leukemia|Multiple Myeloma Oncoethix GmbH December 14 2012 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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