CHMFL-ABL-053

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CHMFL-ABL-053 是一种有效的、选择性的、口服的 Bcr-Abl/Src/p38 激酶抑制剂，IC50 为 70/62/90 nM。

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.

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.

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

ABL-053

Angiogenesis

Bcr-Abl

Bcr-Abl

——

——

1808287-83-3

549.558

C28H26F3N7O2

>98% (HPLC)

——

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

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

(-20℃)

With Ice Pack

≥ 2 years