CCS-1477 (CBP-IN-1)

For research use only.

Catalog No.S9667 Synonyms: CBP-IN-1, CBP/p300-IN-4

CCS-1477 (CBP-IN-1) Chemical Structure

CAS No. 2222941-37-7

CCS1477(CBP-IN-1, CBP/p300-IN-4)is a potent and selective inhibitor of p300/CBP bromodomain. CCS1477 works by inhibiting the expression and function of the androgen receptor (AR), as well as inhibiting c-Myc.

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Biological Activity

Description CCS1477(CBP-IN-1, CBP/p300-IN-4)is a potent and selective inhibitor of p300/CBP bromodomain. CCS1477 works by inhibiting the expression and function of the androgen receptor (AR), as well as inhibiting c-Myc.
Targets
p300/CBP bromodomain [1]
()
androgen receptor [1]
()
c-Myc [1]
()
In vitro

CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases AR- and C-MYC–regulated gene expression.[2]

In vivo

In AR-SV–driven models, CCS1477 has antitumor activity, regulating AR and C-MYC signaling. Early clinical studies suggest that CCS1477 modulates KLK3 blood levels and regulates CRPC biopsy biomarker expression.[2]

Protocol

Cell Research:

[2]

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  • Cell lines: 22Rv1 cells, C4-2 cells
  • Concentrations: 500 nM, 96 nM
  • Incubation Time: 5 hr, 24 hr
  • Method:

    22Rv1 and C4-2 cells are plated in hormone-deficient media for 72 hours, following which cells are treated with vehicle (0 nmol/L) or CCS1477 500 nmol/L for 5 hours, followed by the addition of 10 nmol/L dihydrotestosterone for 3 hours. Then ChIP is performed. 22Rv1 cells are seeded at equal density in hormone-deficient media. After 72 hours, cells are treated with either vehicle control, 100 nmol/L JQ1, or 96 nmol/L CCS1477. After 24 hours, cells are harvested and lysed, and RNA is extracted using TRIzol, per the manufacturer's instructions.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: male CD1 mice
  • Dosages: 3 mg/kg, 30 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (187.05 mM)
Water Insoluble
Ethanol '''''''100 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 534.60
Formula

C30H32F2N4O3

CAS No. 2222941-37-7
Storage powder
in solvent
Synonyms CBP-IN-1, CBP/p300-IN-4
Smiles CC1=C(C(=NO1)C)C2=CC3=C(C=C2)N(C(=N3)C4CCCC(=O)N4C5=CC(=C(C=C5)F)F)C6CCC(CC6)OC

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04068597 Recruiting Drug: CCS1477 Haematological Malignancy|Acute Myeloid Leukemia|Non Hodgkin Lymphoma|Multiple Myeloma CellCentric Ltd. August 9 2019 Phase 1|Phase 2
NCT03568656 Recruiting Drug: CCS1477|Drug: Abiraterone acetate|Drug: Enzalutamide Metastatic Castration-Resistant Prostate Cancer|Advanced Solid Tumors CellCentric Ltd. July 23 2018 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Epigenetic Reader Domain Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID