CHZ868

CHZ868

Identifiers
IUPAC name N-[4-[2-(2,4-difluoroanilino)-1,4-dimethylbenzimidazol-5-yl]oxypyridin-2-yl]acetamide
CAS Number	1895895-38-1
PubChem CID	91885989
ChemSpider	57876249
ChEBI	CHEBI:90828
Chemical and physical data
Formula	C22H19F2N5O2
Molar mass	423.424 g·mol−1
3D model (JSmol)	Interactive image
SMILES CC1=C(C=CC2=C1N=C(N2C)NC3=C(C=C(C=C3)F)F)OC4=CC(=NC=C4)NC(=O)C
InChI 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

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

• Fedratinib
• Pacritinib

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.