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Description: BET bromodomain inhibitor; orally bioavailable
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)
Biological Activity
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
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
| 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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 49.2 | 100 | |
| ethanol | 9.84 | 20 |
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 the degree 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 |
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Product Datasheets
References
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, Bromodomains, 6181, Tocris Bioscience
Citations 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
A collection of over 750 products for cancer research, the guide includes research tools for the study of:
- Cancer Metabolism
- Epigenetics in Cancer
- Receptor Signaling
- Cell Cycle and DNA Damage Repair
- Angiogenesis
- Invasion and Metastasis
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
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
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.