C??H??F?N?OS Molecular Weight:
Protein Tyrosine Kinase/RTK Storage:Please store the product under the recommended conditions in the COA.BIOLOGICAL ACTIVITY
Description CHMFL-ABL-121 is a highly potent type II ABL kinase inhibitor with IC 50s of 2 nM and 0.2 nM against purified inactive
ABL wt and T315I kinase protein, respectively .
IC?? & Target ABL wt
2 nM (IC 50)
In Vitro 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 .
CHMFL-ABL-121 induces apoptosis and arrests cell cycle at G0/G1 phase .
. 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.
Caution: Product has not been fully validated for medical applications. For research use only.
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Product Data Sheet
Inhibitors ?Agonists ?Screening Libraries