OTX015 is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4.
|Source||Oncotarget (2017). Figure 1. OTX015|
|Cell Lines||TNBC cell|
|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 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.|
|Animal models||anti-lymphoma activity NOD-SCID mice|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 55 mg/mL|
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