Cas No.: | 1380087-89-7 |
Chemical Name: | CPI-0610 |
Synonyms: | CPI-0610 |
SMILES: | ClC1=CC=C(C2=N[C@@]([H])(CC(O)=N)C3ON=C(C)C=3C3=CC=CC=C23)C=C1 |
Formula: | C20H16ClN3O2 |
M.Wt: | 365.812943458557 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | 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. |
Target: | Bromodomains |
In Vivo: | 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] |
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. |