For research use only.
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.
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|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.|
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.
|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.|
|In vitro||DMSO||73 mg/mL (199.55 mM)|
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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|NCT02986919||Withdrawn||Drug: CPI-0610||Peripheral Nerve Tumors||University of Texas Southwestern Medical Center||May 5 2017||Phase 2|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|
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