CHZ868

Category:Articles with short descriptionCategory:Short description matches Wikidata Category:Articles with short descriptionCategory:Short description is different from Wikidata
CHZ868
Identifiers
  • N-[4-[2-(2,4-difluoroanilino)-1,4-dimethylbenzimidazol-5-yl]oxypyridin-2-yl]acetamide
CAS Number
PubChem CID
ChemSpider
ChEBI
Chemical and physical data
FormulaC22H19F2N5O2
Molar mass423.424 g·mol−1
3D model (JSmol)
  • CC1=C(C=CC2=C1N=C(N2C)NC3=C(C=C(C=C3)F)F)OC4=CC(=NC=C4)NC(=O)C
  • InChI=1S/C22H19F2N5O2/c1-12-19(31-15-8-9-25-20(11-15)26-13(2)30)7-6-18-21(12)28-22(29(18)3)27-17-5-4-14(23)10-16(17)24/h4-11H,1-3H3,(H,27,28)(H,25,26,30)
  • Key:KQQLBXFPTDVFAJ-UHFFFAOYSA-N
Category:Infobox drug articles with non-default infobox title#%20Category:Chemical pages without DrugBank identifier#*Category:Articles without KEGG source#*Category:Articles without UNII source#*Category:Drugs missing an ATC codeCategory:Drugs with no legal statusCategory:Articles containing unverified chemical infoboxes#*

CHZ868 is a drug which acts as a Janus kinase inhibitor selective for the JAK2 subtype. It was one of the first Janus kinase inhibitors developed, originally for the treatment of leukemia and related blood cancers, and while it did not get approved for clinical use, it is still used for research in the area.[1][2][3][4]

See also

References

  1. ↑ Meyer SC, Keller MD, Chiu S, Koppikar P, Guryanova OA, Rapaport F, et al. (July 2015). "CHZ868, a Type II JAK2 Inhibitor, Reverses Type I JAK Inhibitor Persistence and Demonstrates Efficacy in Myeloproliferative Neoplasms". Cancer Cell. 28 (1): 15–28. doi:10.1016/j.ccell.2015.06.006. PMC 4503933. PMID 26175413.
  2. ↑ Kong X, Sun H, Pan P, Li D, Zhu F, Chang S, et al. (August 2017). "How Does the L884P Mutation Confer Resistance to Type-II Inhibitors of JAK2 Kinase: A Comprehensive Molecular Modeling Study". Scientific Reports. 7 (1): 9088. Bibcode:2017NatSR...7.9088K. doi:10.1038/s41598-017-09586-3. PMC 5567357. PMID 28831147.
  3. ↑ Nair PC, Piehler J, Tvorogov D, Ross DM, Lopez AF, Gotlib J, Thomas D (September 2023). "Next-Generation JAK2 Inhibitors for the Treatment of Myeloproliferative Neoplasms: Lessons from Structure-Based Drug Discovery Approaches". Blood Cancer Discovery. 4 (5): 352–364. doi:10.1158/2643-3230.BCD-22-0189. PMC 10472187. PMID 37498362.
  4. ↑ Codilupi T, Szybinski J, Arunasalam S, Jungius S, Dunbar AC, Stivala S, et al. (February 2024). "Development of Resistance to Type II JAK2 Inhibitors in MPN Depends on AXL Kinase and Is Targetable". Clinical Cancer Research. 30 (3): 586–599. doi:10.1158/1078-0432.CCR-23-0163. PMC 10831334. PMID 37992313.
Category:Non-receptor tyrosine kinase inhibitors Category:Janus kinase inhibitors Category:Fluoroarenes Category:Anilines Category:Benzimidazoles Category:Disubstituted pyridines Category:Acetamides Category:Guanidines
Category:Acetamides Category:All stub articles Category:Anilines Category:Articles containing unverified chemical infoboxes Category:Articles with short description Category:Articles without KEGG source Category:Articles without UNII source Category:Benzimidazoles Category:Chemical pages without DrugBank identifier Category:Disubstituted pyridines Category:Drugs missing an ATC code Category:Drugs with no legal status Category:Fluoroarenes Category:Guanidines Category:Infobox drug articles with non-default infobox title Category:Janus kinase inhibitors Category:Non-receptor tyrosine kinase inhibitors Category:Pharmacology stubs Category:Short description is different from Wikidata Category:Short description matches Wikidata