CPI-0610

CPI-0610
Identifiers
	IUPAC name 2-[(4S)-6-(4-chlorophenyl)-1-methyl-4H-[1,2]oxazolo[5,4-d][2]benzazepin-4-yl]acetamide;
CAS Number	1380087-89-7;
PubChem CID	57389999;
ChemSpider	32738784;
UNII	U4017GUQ06;
Chemical and physical data
Formula	C20H16ClN3O2
Molar mass	365.82 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=NOC2=C1C3=CC=CC=C3C(=N[C@H]2CC(=O)N)C4=CC=C(C=C4)Cl;
	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; Key:GCWIQUVXWZWCLE-INIZCTEOSA-N;

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]

References

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.
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.
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.
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.

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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.