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CPI0610 1380087-89-7

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Synonyms ：
Appearance ：
white powder
Chemical Formula ：
C20H16ClN3O2
Solubility ：
Molecular Weight ：
365.81
Storage and Stability ：
in stock
CAS No. ：
1380087-89-7
Purity ：
99.5%
Introduction
CPI-0610 is a potent, selective, and cell-active BET bromodomain inhibitor CPI-0610 inhibits BRD4-BD1 with IC50 of 39 nM in time-resolved fluorescence energy transfer (TR-FRET ) binding assay. IC50 value: 39 nM Target: Bromodomains 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.in vivo: The t1/2 of CPI-0610 for the rat and dog is 0.93 and 9 h, respectively.

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