CPI-0610, BET bromodomain inhibitor (ab230374)

Overview

  • Product name

    CPI-0610, BET bromodomain inhibitor
  • Description

    Potent, selective BET bromodomain inhibitor
  • Biological description

    Potent, selective benzoisoxazoloazepine bromodomain and extra terminal domain (BET) protein family inhibitor with similar potencies for BRD2, BRD3, BRD4, and BRDT bromodomains (18-220 nM) in an immunoassay. No activity against other bromodomain family members. Reduces transcription of MYC (EC50 = 180 nM). Arrests the cell cycle in the G1 transition and induces caspase-dependent apoptosis in multiple myeloma cells.

  • Purity

    > 98%
  • CAS Number

    1380087-89-7
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    2-[6-(4-Chlorophenyl)-1-methyl-4H-[1,2]oxazolo[5,4-d][2]benzazepin-4-yl]acetamide

  • Molecular weight

    365.82
  • Molecular formula

    C20H16ClN3O2
  • PubChem identifier

    76534645
  • Storage instructions

    Shipped at 4°C. Store at -20°C.
  • Solubility overview

    Soluble in organic solvents such as chloroform, DMSO, and dimethyl formamide, purged with an inert gas. Slightly soluble in aqueous buffers if first dissolved in DMSO and then diluted with the aqueous buffer.

  • SMILES

    CC1=NOC2=C1C3=CC=CC=C3C(=NC2CC(=O)N)C4=CC=C(C=C4)Cl
  • Source

    Synthetic

References

This product has been referenced in:

  • Siu KT  et al. Preclinical activity of CPI-0610, a novel small-molecule bromodomain and extra-terminal protein inhibitor in the therapy of multiple myeloma. Leukemia 31:1760-1769 (2017). Read more (PubMed: 27890933) »
  • Albrecht BK  et al. Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials. J Med Chem 59:1330-9 (2016). Read more (PubMed: 26815195) »

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