OTX015 （MK 8628/Birabresib）
Molecular Weight(MW): 491.99
OTX015 is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays. Phase 1.
Cited by 5 Publications
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F, Representative histologic images of the individual treatments of the xenografts performed in C. Slides were stained with hematoxylin and eosin (HE).
Clin Cancer Res, 2018, doi: 10.1158/1078-0432.CCR-18-1040. OTX015 （MK 8628/Birabresib） purchased from Selleck.
LN229, U87, NCH644, or GBM14 cells were treated with indicated drugs and analyzed for levels of the indicated proteins by conventional Western blotting or capillary electrophoresis. All concentrations are in μmol/L. Blots or capillary electrophoresis were quantified for the levels of Mcl-1 and Noxa normalized with its related loading control.
Clin Cancer Res, 2018, 24(16):3941-3954. OTX015 （MK 8628/Birabresib） purchased from Selleck.
A. Growth inhibition IC50 values of CUDC-907 and three BET inhibitors (I-BET-762, JQ1, and OTX015) in three BRD–NUT fusion-positive NMC cell lines. Cell viability after 72-hour incubation was assessed by the CellTiter-Glo assay. Growth inhibition IC50 values for each compound were determined by GraphPad Prism 5.
Mol Cancer Ther, 2016, 16(4 suppl 1):S263-S276. OTX015 （MK 8628/Birabresib） purchased from Selleck.
C11 cells were mock-treated or treated with either OTX015 (0.01 μM), prostratin (0.2 μM), or OTX015 (0.01 μM)/prostratin (0.2 μM). The effect of activation of the HIV-1 promoter was determined by quantifying GFP-positive cells 48 hours after treatment using flow cytometry. A summary of the activation assays is presented as a series of histograms.
Sci Rep, 2016, 6:24100. OTX015 （MK 8628/Birabresib） purchased from Selleck.
Purity & Quality Control
Choose Selective Epigenetic Reader Domain Inhibitors
|Description||OTX015 is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays. Phase 1.|
|Features||Orally bioavailable BRD2/3/4-selective inhibitor that has been tested in Phase I clinical trials for treatment of Haematological Malignancies.|
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.  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. 
|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. |
TR-FRET Assay :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.
|In vitro||DMSO||98 mg/mL (199.19 mM)|
|Ethanol||98 mg/mL (199.19 mM)|
|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.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02303782||Withdrawn||Acute Myeloid Leukemia||Oncoethix GmbH||January 2015||Phase 1|Phase 2|
|NCT01713582||Completed||Acute Myeloid Leukemia|Diffuse Large B-cell Lymphoma|Acute Lymphoblastic Leukemia|Multiple Myeloma||Oncoethix GmbH||December 14 2012||Phase 1|
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.
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