2270879-07-5

2270879-07-5 structure

2270879-07-5 structure

Name: CHMFL-ABL-121
Chemical Name: CHMFL-ABL-121
CAS Number: 2270879-07-5
Molecular Formula: C₃₀H₃₁F₃N₆OS
Molecular Weight: 580.67
Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Bcr-Abl
Create Date: 2019-07-01 07:06:15
Modify Date: 2024-01-24 10:31:22
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].

Name	CHMFL-ABL-121

Description	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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Bcr-Abl
Target	ABL wt:2 nM (IC50)
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[1]. CHMFL-ABL-121 induces apoptosis and arrests cell cycle at G0/G1 phase[1].
References	[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.

Molecular Formula	C₃₀H₃₁F₃N₆OS
Molecular Weight	580.67