CCS 1477

Key Product Details

Product Description

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.

Licensing Information

Sold under license from CellCentric Ltd

Product Specifications for CCS 1477

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for CCS 1477

The following data is based on the product molecular weight 534.61.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

1 Recalculate

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.87 mL	9.35 mL	18.71 mL
5 mM	0.37 mL	1.87 mL	3.74 mL
10 mM	0.19 mL	0.94 mL	1.87 mL
50 mM	0.04 mL	0.19 mL	0.37 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Welti Targeting the p300/CBP axis in lethal prostate cancer. Cancer Discov. 2021 PMID: 33431496
• Nicosia Therapeutic targeting of EP300/CBP by bromodomain inhibition in hematologic malignancies. Cancer Cell 2023 PMID: 37995682

Product Documents for CCS 1477