CPI-0610 is a drug which acts as a BET inhibitor, mainly acting at the BRD2 and BRD4 subtypes. It has potential applications in the treatment of various forms of cancer.[1][2][3][4]

CPI-0610
Identifiers
  • 2-[(4S)-6-(4-chlorophenyl)-1-methyl-4H-[1,2]oxazolo[5,4-d][2]benzazepin-4-yl]acetamide
CAS Number
PubChem CID
ChemSpider
UNII
ChEBI
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC20H16ClN3O2
Molar mass365.82 g·mol−1
3D model (JSmol)
  • CC1=NOC2=C1C3=CC=CC=C3C(=N[C@H]2CC(=O)N)C4=CC=C(C=C4)Cl
  • 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
  • Key:GCWIQUVXWZWCLE-INIZCTEOSA-N

References

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  1. ^ Albrecht BK, Gehling VS, Hewitt MC, Vaswani RG, Côté A, Leblanc Y, et al. (February 2016). "Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials". Journal of Medicinal Chemistry. 59 (4): 1330–9. doi:10.1021/acs.jmedchem.5b01882. PMID 26815195.
  2. ^ Zhao L, Okhovat JP, Hong EK, Kim YH, Wood GS (January 2019). "Preclinical Studies Support Combined Inhibition of BET Family Proteins and Histone Deacetylases as Epigenetic Therapy for Cutaneous T-Cell Lymphoma". Neoplasia. 21 (1): 82–92. doi:10.1016/j.neo.2018.11.006. PMC 6280696. PMID 30529073.
  3. ^ Raythatha J, Arnold L (November 2019). "The future of epigenetic therapy: CPI-0610 for the treatment of myeloidfibrosis". Epigenomics. 11 (14): 1553–1555. doi:10.2217/epi-2019-0274. PMID 31729905.
  4. ^ Bankar A, Gupta V (April 2020). "Investigational non-JAK inhibitors for chronic phase myelofibrosis". Expert Opinion on Investigational Drugs. 29 (5): 461–474. doi:10.1080/13543784.2020.1751121. PMID 32245330.