CHMFL-ABL-121

CHMFL-ABL-121 is a highly potent type II ABL kinase inhibitor with IC50s of 2 nM and 0.2 nM against purified inactive ABL wt and T315I kinase protein, respectively[1].

Research Areas >> Cancer

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Bcr-Abl

ABL wt:2 nM (IC50)

CHMFL-ABL-121 dose-dependently inhibits BCRABL's auto-phosphorylation at Y245 site in K562 (EC50 < 10 nM),MEG-01 (EC50 < 10 nM) and KU812 (EC50 < 30 nM) cells and also significantly blocks the phosphorylation of downstream signaling mediators STAT5, CrkL and ErK[1]. CHMFL-ABL-121 induces apoptosis and arrests cell cycle at G0/G1 phase[1].

[1]. Liu X, et al. Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants including T315I for chronic myeloid leukemia. Eur J Med Chem. 2018 Dec 5;160:61-81.