All AbMole products are for research use only, cannot be used for human consumption.
OTX015 is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4.
NPJ Precis Oncol. 2023 Jan 24;7(1):11.
Towards precision radiation oncology: endocrine therapy response as a biomarker for personalization of breast radiotherapy
OTX015 (Birabresib) purchased from AbMole
JCI Insight. 2022 May 9;7(9):e152955.
Targeting radioresistance and replication fork stability in prostate cancer
OTX015 (Birabresib) purchased from AbMole
JCI Insight. 2022 Sep 8;7(17):e151851.
Targeting ESR1 mutation-induced transcriptional addiction in breast cancer with BET inhibition
OTX015 (Birabresib) purchased from AbMole
 |
Source | Oncotarget (2017). Figure 1. OTX015 |
| Method | cell | |
| Cell Lines | TNBC cell | |
| Concentrations | 0.8 mg/ml | |
| Incubation Time | 24, 48 and 72 h | |
| Results | OTX015 induced an increase in the percentage of cells in the G1 phase after 24 h of treatment, maintained throughout the 72-h exposure |
| Cell Experiment | |
|---|---|
| Cell lines | 33 cell lines from mature B-cell lymphoid tumors |
| Preparation method | We first evaluated the anti-proliferative activity of the BET Bromodomain-inhibitor OTX015 in a panel of 33 cell lines derived from mature B-cell lymphoid tumors. As assessed by MTT assays performed after 72 hours of drug exposure, OTX015 was active in a dose-dependent manner in almost all the cell lines (Fig. 1A), at concentrations achievable in the clinical setting. |
| Concentrations | 70nM~15µM |
| Incubation time | 72h |
| Animal Experiment | |
|---|---|
| Animal models | anti-lymphoma activity NOD-SCID mice |
| Formulation | unknown |
| Dosages | 25 mg/kg |
| Administration | oral gavage |
| Molecular Weight | 491.99 |
| Formula | C25H22ClN5O2S |
| CAS Number | 202590-98-5 |
| Solubility (25°C) | DMSO 49 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] Mingzhu Yin, et al. Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction
[4] Jixiang Shi, et al. Potent Activity of the Bromodomain Inhibitor OTX015 in Multiple Myeloma
| Related Epigenetic Reader Domain Products |
|---|
| RVX-208
Apabetalone (RVX-208) is a first-in-class, small molecule inhibitor of BET bromodomain with IC50 of 0.51 μM for BD2. |
| I-BET151
I-BET151 (GSK1210151A) is an inhibitor of the BET family with IC50 of 0.5 μM, 0.25 μM and 0.79 μM for BRD2, BRD3 and BRD4, respectively. |
| (+)-JQ1
(+)-JQ1 is a BET bromodomain inhibitor that acts on BRD4(2) with an IC50 of 33 nM and binds to all bromodomain domains in the BET family, but not to bromodomain domains outside the BET family. JQ1 down-regulates CD47 expression through a C-MYC-mediated pathway, and JQ1 down-regulates CD47 expression through a C-MYC-mediated pathway. |
| I-BET-762
I-BET-762 (GSK525762) is a selective small molecule BET inhibitor. |
| CPI-0610
CPI-0610 is a novel BET protein bromodomain inhibitor. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
