Pelabresib (CPI-0610) is a potent and selective BET bromine-domain protein inhibitor with an IC50 value of 39 nM for BRD4-BD1 in TR-FRET assay. It is currently in clinical trials for the treatment of hematologic malignancies. CPI-0610 inhibited target gene expression of Nuclear receptor binding SET domain protein 3 (NSD3).

 

Brand: BCM

 

Target: c-Myc; Epigenetic Reader Domain

 

Signaling Pathways: Cell Cycle/Checkpoint; Chromatin/Epigenetic

 

In Vitro: CPI-0610 can inhibit the growth of multiple myeloma cells in the presence of cytokines and co-culture with bone marrow stromal cells. CPI-0610 can induce apoptosis and late G1 cell arrest associated with MYC downregulation. Then, the levels of BCL2, NF-κB and MCL1 proteins in the multiple myeloma cells did not change. CPI-0610 inhibited the expression of Ikaros and IRF4 in multiple myeloma cells at transcriptional and protein levels.

 

pKa: 16.07±0.40(Predicted)

 

Solubility: Soluble in DMSO; soluble in Ethanol. Insoluble in Water.

 

Isomeric SMILES: CC1=NOC2=C1C3=CC=CC=C3C(=N[C@H]2CC(=O)N)C4=CC=C(C=C4)Cl  

 

InChIKey: GCWIQUVXWZWCLE-INIZCTEOSA-N  

 

InChI: InChI=1S/C20H16ClN3O2/c1-11-18-14-4-2-3-5-15(14)19(12-6-8-13(21)9-7-12)23-16(10-17(22)25)20(18)26-24-11/h2-9,16H,10H2,1H3,(H2,22,25)/t16-/m0/s1

 

Attribute
[Chem Name]	2-[(4S)-6-(4-chlorophenyl)-1-methyl-4H-[1,2]oxazolo[5,4-d][2]benzazepin-4-yl]acetamide
[Synonym]	Pelabresib; CPI-0610
[CAS No.]	1380087-89-7
[Formula]	C20H16ClN3O2
[Molecular]	365.81
[Form]	Solid Powder
[Storage]	Store at -20°C

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