CPI-0610
Modify Date: 2024-01-02 17:54:00
CPI-0610 structure
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Common Name | CPI-0610 | ||
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| CAS Number | 1380087-89-7 | Molecular Weight | 365.813 | |
| Density | 1.4±0.1 g/cm3 | Boiling Point | 622.8±55.0 °C at 760 mmHg | |
| Molecular Formula | C20H16ClN3O2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 330.5±31.5 °C | |
Use of CPI-0610CPI-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 nMTarget: 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.[1] in vivo: The t1/2 of CPI-0610 for the rat and dog is 0.93 and 9 h, respectively.[1] |
| Name | 2-[(4S)-6-(4-Chlorophenyl)-1-methyl-4H-[1,2]oxazolo[5,4-d][2]benzazepin-4-yl]acetamide |
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| Synonym | More Synonyms |
| 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. IC50 value: 39 nMTarget: 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.[1] in vivo: The t1/2 of CPI-0610 for the rat and dog is 0.93 and 9 h, respectively.[1] |
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| Related Catalog | |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 622.8±55.0 °C at 760 mmHg |
| Molecular Formula | C20H16ClN3O2 |
| Molecular Weight | 365.813 |
| Flash Point | 330.5±31.5 °C |
| Exact Mass | 365.093109 |
| LogP | 2.72 |
| Vapour Pressure | 0.0±1.8 mmHg at 25°C |
| Index of Refraction | 1.692 |
| Storage condition | 2-8℃ |
| 4H-Isoxazolo[5,4-d][2]benzazepine-4-acetamide, 6-(4-chlorophenyl)-1-methyl-, (4S)- |
| 2-[(4S)-6-(4-Chlorophenyl)-1-methyl-4H-[1,2]oxazolo[5,4-d][2]benzazepin-4-yl]acetamide |
| BET bromodomain inhibitor |
| CPI-0610 |