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CPI-0610

Chemical Structure : CPI-0610

CAS No.: 1845726-14-8

CPI-0610 (Pelabresib, CPI0610)

Catalog No.: PC-62282Not For Human Use, Lab Use Only.

Pelabresib (CPI-0610) is a potent, selective, and cell-active BET bromodomain inhibitor with IC50 of 39 nM for BRD4-BD1 in TR-FRET assay.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Pelabresib (CPI-0610) is a potent, selective, and cell-active BET bromodomain inhibitor with IC50 of 39 nM for BRD4-BD1 in TR-FRET assay.
Pelabresib (CPI-0610) is a shows remarkably selectivity, over the bromodomains of CBP, BRD9, BRPF1, PCAF, BRG1, ATAD2, TRIM24, BRD8.
Pelabresib (CPI-0610) is a has an IC50 of 0.18 uM in MYC RNA expression assay.
Pelabresib (CPI-0610) is a demonstrates antitumor efficacy in an MV-4-11 mouse xenograft model.

Physicochemical Properties

M.Wt 365.817
Formula C20H16ClN3O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[e]isoxazolo[5,4-c]azepin-4-yl)acetamide

References

1. Albrecht BK, et al. J Med Chem. 2016 Feb 25;59(4):1330-9.

2. Siu KT, et al. Leukemia. 2017 Jan 3. doi: 10.1038/leu.2016.355.

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