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2885162-99-0

2885162-99-0 Structure

2885162-99-0 Structure
IdentificationBack Directory
[Name]

I-BET282E
[CAS]

2885162-99-0
[Synonyms]

Hazard InformationBack Directory
[Uses]

I-BET282E is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282E shows pIC50s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD)[1].
[in vivo]

I-BET282E (Male CD1 Mice; 3 mg/kg-p.o.; 1 mg/kg-i.v.) treatment shows the Clb, LBF, Vss, t1/2 (i.v.), and F values of 23 mL/min/kg, 19%, 1.9 L/kg, and 51%, respectively[1].
I-BET282E (Male Wistar Han Rats; 1 mg/kg; p.o.) treatment shows the AUC0-t, Cmax and Tmax values of 467 ng h/mL, 125 ng/mL, and 1 hour, respectively[1].

[References]

[1] Jones KL, et al. Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression. J Med Chem. 2021;64(16):12200-12227. DOI:10.1021/acs.jmedchem.1c00855
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