The t1/2 of CPI-0610 for the rat and dog is 0.93 and 9 h, respectively.[1]
In Vitro
CPI-0610 is about 6 times more potent against BET BD-2 than against BET BD-1. When tested on other members of the bromodomain family, CPI-0610 is remarkably selective, displaying essentially no activity in TR-FRET- or AlphaLisa-based assays against the bromodomains of CBP, BRD9, BRPF1, PCAF, BRG1, ATAD2, TRIM24, BRD8 (IC50 of >20 μM, >80 μM, >20 μM, >20 μM, >20 μM, >80 μM, >20 μM, and >15 μM, respectively), among others. In a CEREP express panel of about 50 GPCRs, ion channels, and transporters, the compound displayed no meaningful inhibition. CPI-0610 also displays negligible inhibition of cytochrome P450 activity when tested at 10 μM against a number of common isoforms, and it also showed no time-dependent inhibition.[1]
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Albrecht BK, et al. Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials. J Med Chem. 2016 Feb 25;59(4):1330-9.
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