CHMFL-ABL-053( ABL-053 )

Catalog No. M12768 CAS No. 1808287-83-3

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Product Name

CHMFL-ABL-053
Note

Research use only, not for human use.
Brief Description

CHMFL-ABL-053 is a potent, selective and orally available Bcr-Abl/Src/p38 kinase inhibitor with IC50 of 70/62/90 nM.
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.
In Vitro

CHMFL-ABL-053 (Compound 18a) inhibits the proliferation of CML cell lines with GI50 of 14, 25 and 16 nM against K562, KU812 and MEG-01, respectively.
In Vivo

CHMFL-ABL-053 (Compound 18a) (50 mg/kg/day) almost completely suppresses tumor progression in the K562 cells inoculated xenograft mouse model.
Synonyms

ABL-053
Pathway

Angiogenesis
Target

Bcr-Abl
Recptor

Bcr-Abl
Research Area

——
Indication

——

CAS Number

1808287-83-3
Formula Weight

549.558
Molecular Formula

C28H26F3N7O2
Purity

>98% (HPLC)
Solubility

——
SMILES

O=C(C1=CN=C(NC2=CC=C(C)C(N)=C2)N=C1NC)NC3=CC(NC(C4=CC=CC(C(F)(F)F)=C4)=O)=CC=C3C
Chemical Name

2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide

1. Liang X, et al. J Med Chem. 2016 Mar 10;59(5):1984-2004.

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