CCS-1477

Based on 9 reference(s) in Google Scholar 8 10 9

Axon 3933

CAS [2222941-37-7]

MF C30H32F2N4O3
MW 534.60

  • Purity: 99%
  • Optical purity: 99%
  • Soluble in DMSO

CCS-1477

Description

CCS-1477 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). 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, which represents a new therapeutic option for prostate cancer patients who have progressed after failure of anti-androgen therapy and in combination with anti-androgens such as enzalutamide or abiraterone.

KEYWORDS: CCS-1477 | Supplier | p300 and CBP Bromodomain inhibitor | CCS1477 | CCS 1477 | CT-CCS1477 | CAS [2222941-37-7] | Androgen Receptor (AR) | P300 | CBP | Inhibitor | Proteins

The purity of Axon Ligands™ is confirmed by HPLC-MS, 1H-NMR and/or microanalysis. Analytical data are available upon request.

Caution: Axon Ligands™ are not fully tested. They are for research purposes only! Not for human consumption!

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