Pelabresib (CPI-0610)

For research use only.

Catalog No.S7853

1 publication

Pelabresib (CPI-0610) Chemical Structure

CAS No. 1380087-89-7

Pelabresib (CPI-0610) is a potent and selective benzoisoxazoloazepine BET bromodomain inhibitor with an IC50 of 39 nM for BRD4-BD1 in TR-FRET assay and currently undergoing human clinical trials for hematological malignancies. CPI-0610 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.

Selleck's Pelabresib (CPI-0610) has been cited by 1 publication

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Biological Activity

Description Pelabresib (CPI-0610) is a potent and selective benzoisoxazoloazepine BET bromodomain inhibitor with an IC50 of 39 nM for BRD4-BD1 in TR-FRET assay and currently undergoing human clinical trials for hematological malignancies. CPI-0610 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.
Targets
BRD4-BD1 [1]
(Cell-free assay)
MYC [1]
(in MV-4-11 cells)
39 nM 180 nM(EC50)
In vitro

CPI-0610 inhibits MM(multiple myeloma) cell growth in the presence of cytokines and when co-cultured with bone marrow stromal cells. CPI-0610 induces apoptosis and G1 cell cycle arrest associated with MYC downregulation. However, protein levels of BCL2, NF-κB and MCL1 remain unchanged in MM cells upon BET inhibition. CPI-0610 suppresses Ikaros and IRF4 expression at the levels of both transcription and protein in MM cells[2].

In vivo In a mouse xenograft model using MV-4-11 acute myeloid leukemia cells, MYC mRNA levels of CPI-0610-treated mice were substantially reduced at 4 h compared to the vehicle control and recovered toward the control level at the later time points, which corresponded with decreasing free concentrations of compound in plasma. BET bromodomain inhibition by CPI-01610 resulted in substantial suppression of tumor growth over the time period examined (41%, 80%, and 74% tumor growth inhibition, respectively), without any significant body weight loss in the animals. On the basis of an acceptable toxicity profile in rat and dog, A common set of toxicities was observed in both species: lymphoid depletion; hypocellularity of the bone marrow with associated anemia and thrombocytopenia; GI mucosal atrophy, erosion, and ulceration; degeneration of the testicular seminiferous epithelium; and mild to moderate hyperglycemia. These toxicities is reversible[1].

Protocol

Cell Research:

[1]

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  • Cell lines: MV-4-11 cells
  • Concentrations: --
  • Incubation Time: 4 h
  • Method:

    MV-4-11 cells were plated at 10,000 cells/well in 96-well plates containing compounds in 100 μL RPMI medium supplemented with 10% FBS. Cells were incubated with compound for 4 hours at 37◦C and 5% CO2 prior to analysis of MYC transcript levels. Inhibition was calculated relative to DMSO treated MYC levels.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Balb/c nude mice with MV-4-11 xenografts
  • Dosages: 10 mg/kg twice daily or 2 mg/kg twice weekly
  • Administration: s.c.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 73 mg/mL (199.55 mM)
Water Insoluble
Ethanol ''''12 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 365.81
Formula

C20H16ClN3O2

CAS No. 1380087-89-7
Storage powder
in solvent
Synonyms N/A
Smiles CC1=NOC2=C1C3=CC=CC=C3C(=NC2CC(=O)N)C4=CC=C(C=C4)Cl

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02986919 Withdrawn Drug: CPI-0610 Peripheral Nerve Tumors University of Texas Southwestern Medical Center May 5 2017 Phase 2
NCT02157636 Completed Drug: CPI-0610 Multiple Myeloma Constellation Pharmaceuticals|The Leukemia and Lymphoma Society July 2014 Phase 1
NCT01949883 Completed Drug: CPI-0610 Lymphoma Constellation Pharmaceuticals|The Leukemia and Lymphoma Society September 2013 Phase 1

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

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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