OTX015 is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4.
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OTX015 (Birabresib) purchased from AbMole
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Targeting radioresistance and replication fork stability in prostate cancer
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Targeting ESR1 mutation-induced transcriptional addiction in breast cancer with BET inhibition
OTX015 (Birabresib) purchased from AbMole
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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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[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
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