OTX 015
Tocris Bioscience, part of Bio-Techne | Catalog # 6181
BET bromodomain inhibitor; orally bioavailable
Key Product Details
Description
BET bromodomain inhibitor; orally bioavailable
Alternative Names
Birabresib
Product Description
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.Product Specifications
Molecular Weight
491.99
Formula
C25H22ClN5O2S
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for OTX 015
For research use only
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