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OTX 015

Cat. No. 6181 Submit a Review Datasheet / COA / SDS
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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 Technical Data Solubility Calculators Datasheets References

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.

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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!

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