Home Epigenetics Epigenetic Reader Domain inhibitor - NSD inhibitor Pelabresib (CPI-0610) For research use only.

Pelabresib (CPI-0610)

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.

Pelabresib (CPI-0610) Chemical Structure

Pelabresib (CPI-0610) Chemical Structure

CAS No. 1380087-89-7

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Pelabresib (CPI-0610) Related Products

Signaling Pathway

Epigenetic Reader Domain Signaling Pathways

Epigenetic Reader Domain Signaling Pathway

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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models mouse xenograft model using MV-4-11 acute myeloid leukemia cells
Dosages 15 mg/kg twice daily
Administration s.c.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05391022 Completed
Advanced Malignancies|Solid Tumor|Hematological Malignancy
Constellation Pharmaceuticals
 July 20 2021 Phase 1
NCT02986919 Withdrawn
Peripheral Nerve Tumors
University of Texas Southwestern Medical Center
 May 5 2017 Phase 2
NCT02157636 Completed
Multiple Myeloma
Constellation Pharmaceuticals|The Leukemia and Lymphoma Society
 July 15 2014 Phase 1
NCT01949883 Completed
Lymphoma
Constellation Pharmaceuticals|The Leukemia and Lymphoma Society
 September 5 2013 Phase 1

Chemical Information & Solubility

Molecular Weight 365.81 Formula

C20H16ClN3O2
CAS No. 1380087-89-7 SDF Download Pelabresib (CPI-0610) SDF
Smiles CC1=NOC2=C1C3=CC=CC=C3C(=NC2CC(=O)N)C4=CC=C(C=C4)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 73 mg/mL ( (199.55 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 12 mg/mL

Water : Insoluble


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