CPI 0610
- Soluble in DMSO
- MF: C20H16ClN3O2
- MW: 365.81
Description
Selective and metabolically stable inhibitor of the BET family of bromodomains (BET-BRD; IC50 values 0.12 - 0.17 µM and 0.22 µM for inhibition of BD-1 of BRD2-4 and BRDT, respectively), demonstrating a correlation between BET-driven reduction in MYC gene expression and tumor growth inhibition in a xenograft study. CPI 0610 displays essentially no activity in TR-FRET- or AlphaLisabased assays against the bromodomains of CBP, BRD9, BRPF1, PCAF, BRG1, ATAD2, TRIM24, BRD8 (IC50 value > 15 µM), and no meaningful inhibition in a CEREP express panel of about 50 GPCRs, ion channels, and transporters.
Note: This item is currently suspended at the request of the developer. You might request a quotation for contract research synthesis. Please contact us for conditions and more detailed information.
More Information
| Parent CAS No. | 1380087-89-7 |
|---|---|
| Chemical Name | 2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[e]isoxazolo[5,4-c]azepin-4-yl)acetamide |
| extra_info | Constellation Pharmaceuticals Inc compound; sold under agreement with Constellation Pharmaceuticals Inc. |
| MFCD | N.A. |
| Short Description | BET-BRD inhibitor |
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