CCS 1477 New

Biological Activity

CCS 1477 is a selective p300/CBP bromodomain inhibitor. CCS 1477 binds with high affinity to p300 and CBP (K_d values are 1.3 and 1.7 nM, respectively), and with 170/130-fold selectivity compared with BRD4 (K_d = 222 nM). In vitro, CCS 1477 inhibits the proliferation of OPM-2 multiple myeloma cells (GI₅₀ = 5 nM). Also, CCS 1477 inhibits cell proliferation in prostate cancer cell lines and decreases AR- and C-MYC-regulated gene expression. In vivo, CCS 1477 significantly improves survival and reduces tumor size in MOLM16 AML and OPM2 myeloma tumors in subcutaneous xenograft models. CCS 1477 is orally bioavailable.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Product Datasheets