CHMFL-ABL-053

Names

[ Name ]:
CHMFL-ABL-053

[Synonym ]:
5-Pyrimidinecarboxamide, 2-[(3-amino-4-methylphenyl)amino]-4-(methylamino)-N-[2-methyl-5-[[3-(trifluoromethyl)benzoyl]amino]phenyl]-
2-[(3-Amino-4-methylphenyl)amino]-4-(methylamino)-N-(2-methyl-5-{[3-(trifluoromethyl)benzoyl]amino}phenyl)-5-pyrimidinecarboxamide

Biological Activity

[Description]:

CHMFL-ABL-053 is a potent, selective and orally available Bcr-Abl/Src/p38 kinase inhibitor with IC50 of 70/62/90 nM; no inhibitory activity against c-Kit (>10 uM); inhibits the proliferation of CML cell lines K562 (GI50=14 nM), KU812 (GI50=25 nM), and MEG-01 (GI50=16 nM); completely suppresses tumor progression in the K562 cells inoculated xenograft mouse model with 50 mg/kg/day dosage treatment.

[References]

References 1. Liang X, et al. J Med Chem. 2016 Mar 10;59(5):1984-2004. View Related Products by Target Bcr-Abl

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C₂₈H₂₆F₃N₇O₂

[ Molecular Weight ]:
549.547

[ Exact Mass ]:
549.210022

[ LogP ]:
4.60

[ Index of Refraction ]:
1.698

Related Compounds

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