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Background Information:
CCS-1477 (CCS1477) is a potent, selective and orally bioavailable inhibitor of the Bromodomain of p300 and CBP, binding to the targets with high affinity (Kd = 1.3/1.7nM) and selectivity (Kd = 222nM; BRD4) (ref 1). E1A binding protein (p300) and CREB binding protein (CBP) are two closely related transcriptional activators of androgen receptor (AR) and its variant forms. CCS-1477 enhances degradation of numerous cellular proteins including the AR and AR variants in prostate cancer cells; Demonstrates potent single-agent efficacy using in vitro and in vivo models of prostate cancer, and enhances the efficacy of Enzalutamide when used in combination. It is currently in clinical evaluation for the treatment of castrate resistant prostate cancer by down-regulation of AR, AR-SV and c-MYC expression and function.
Reference:
1. N. Pegg, et al, Characterization of CCS1477: A novel small molecule inhibitor of p300/CBP for the treatment of castration resistant prostate cancer, Journal of Clinical Oncology 2017 35:15_suppl, 11590-11590.
2. J. S. De Bono, et al, Journal of Clinical Oncology 2019 37:15_suppl, TPS5089-TPS5089.
APIM050321: CCS-1477 (CCS1477)
CAS No.: 2222941-37-7.
Molecular Formula: C30H32 F2N4O3 • 0.5H2O.
Molecular Weight: 534.6.
Purity: >99% Purity by Achiral and Chiral HPLCs.
QC: Achiral and Chiral HPLCs, MS, NMR, and Quantitative Elemental Analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.
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