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OTX015

Cat. No. M2903
OTX015 Structure
Synonym:

MK-8628; Birabresib

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 150 In stock
50mg USD 480 In stock
100mg USD 800 In stock
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Quality Control
Biological Activity

OTX015 is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4.

Customer Product Validations & Biological Datas
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
Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 491.99
Formula C25H22ClN5O2S
CAS Number 202590-98-5
Purity 99.95%
Solubility DMSO 80 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: OTX015, MK-8628; Birabresib supplier, Epigenetic Reader Domain, inhibitors

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