OTX 015

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Description: BET bromodomain inhibitor; orally bioavailable
Alternative Names: Birabresib
Chemical Name: (6S)-4-(4-Chlorophenyl)-N-(4-hydroxyphenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (6)

Biological Activity for OTX 015

OTX 015 is a 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.

Compound Libraries for OTX 015

OTX 015 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for OTX 015

M. Wt 491.99
Formula C25H22ClN5O2S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 202590-98-5
PubChem ID 9936746
InChI Key GNMUEVRJHCWKTO-FQEVSTJZSA-N
Smiles CC1=C(C2=C(N3C(C)=NN=C3[C@@H](N=C2C4=CC=C(C=C4)Cl)CC(NC5=CC=C(C=C5)O)=O)S1)C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for OTX 015

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 49.2 100
ethanol 9.84 20

Preparing Stock Solutions for OTX 015

The following data is based on the product molecular weight 491.99. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

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References for OTX 015

References are publications that support the biological activity of the product.

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, OTX 015 supplier, OTX015, BET, bromodomain, extraterminal, BRD2, BRD3, BRD4, inhibitors, inhibits, leukemia, birabresib, Y803, MK8628, Birabresib, Bromodomains, 6181, Tocris Bioscience

Citations for OTX 015

Citations are publications that use Tocris products.

Currently there are no citations for OTX 015. Do you know of a great paper that uses OTX 015 from Tocris? Please let us know.

Reviews for OTX 015

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Cancer Research Product Guide

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Epigenetics Scientific Review

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Epigenetics Research Bulletin

Epigenetics Research Bulletin

Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:

  • Bromodomains
  • DNA Methyltransferases
  • Histone Deacetylases
  • Histone Demethylases
  • Histone Methyltransferases
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