CHMFL-ABL/KIT-155 is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s: 46 nM/75 nM). It arrests cell cycle progression and induces apoptosis.

Abl (type II):46 nM , Lck:12 nM , DDR1:116 nM , BLK:81 nM , CSF1R:227 nM , PDGFRβ:80 nM , DDR2:325 nM , c-Kit:75 nM

CHMFL-ABL/KIT-155 also presents significant inhibitory activities to BLK, CSF1R, DDR1, DDR2, LCK and PDGFRβ (IC50s: 81 nM, 227 nM, 116 nM, 325 nM,12 nM, and 80 nM) kinases. CHMFL-ABL/KIT-155 exhibits anti-proliferation activities in the BCR-ABL dependent CML cancer cell lines such as MEG-01 (GI50: 0.02 μM), K562 (GI50: 0.027 μM), and KU812 (GI50: 0.056 μM). It also potently inhibits the growth of c-KIT dependent GISTs cancer cell lines including GIST-882 (GI50: 0.095 μM), GIST-T1 (GI50: 0.023 μM) but not c-KIT independent GIST-48B (GI50: 3.96 μM).

In female nu/nu mice bearing established K562 tumor xenografts, CHMFL-ABL/KIT-155 (25-100 mg/kg; p.o.; once daily for 28 days) shows dose-dependent tumor progression suppression without apparent toxicity.