BET bromodomain inhibitor (IC50 values are in the range 92 - 112 nM). Inhibits proliferation and induces apoptosis of leukemia cell lines in vitro. Decreases BRD2, BRD4 and c-MYC protein expression. Orally bioavailable.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 491.99. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.03 mL||10.16 mL||20.33 mL|
|5 mM||0.41 mL||2.03 mL||4.07 mL|
|10 mM||0.2 mL||1.02 mL||2.03 mL|
|50 mM||0.04 mL||0.2 mL||0.41 mL|
References are publications that support the products' biological activity.
Berenguer-Daizé et al (2016) OTX015 (MK-8628), a novel BET inhibitor, displays in vitro and in vivo antitumor effects alone and in combination with conventional therapies in glioblastoma models. Int.J.Cancer 139 2047 PMID: 27388964
Coudé et al (2015) BET inhibitor OTX015 targets BRD2 and BRD4 and decreases c-MYC in acute leukemia cells. Oncotarget 6 17698 PMID: 25989842
If you know of a relevant reference for OTX 015, please let us know.
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Keywords: OTX 015, supplier, OTX015, BET, bromodomain, extraterminal, BRD2, BRD3, BRD4, inhibitors, inhibits, leukemia, Bromodomains, Bromodomains, Tocris Bioscience
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