OTX 015

Name: OTX 015
Brand: Tocris Bioscience
SKU: 6181

Tocris Bioscience, part of Bio-Techne | Catalog # 6181

Citations (3)

COA / SDS

BET bromodomain inhibitor; orally bioavailable

Key Product Details

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)
Molecular Weight:	491.99

View Full Technical Details for OTX 015

Technical Data
Citations

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 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 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.

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	0.20 mL	1.02 mL	2.03 mL
50 mM	0.04 mL	0.20 mL	0.41 mL

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References for OTX 015

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

Coudé BET inhibitor OTX015 targets BRD2 and BRD4 and decreases c-MYC in acute leukemia cells. Oncotarget 2015 PMID: 25989842
Berenguer-Daizé 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 2016 PMID: 27388964