Comparison of effects of the tyrosine kinase inhibitors AG957, AG490, and STI571 on BCR-ABL - Expressing cells, demonstrating synergy between AG490 and STI571

Abstract

STI571 (formerly CGP57148) and AG957 are small molecule inhibitors of the protein tyrosine kinase (PTK) p145abl and its oncogenic derivative p210bcr-abl. AG490 is an inhibitor of the PTK Janus kinase 2 (JAK2). No direct comparison of these inhibitors has previously been reported, so this study compared their effects on factor-dependent FDC-P1,32D, and MO7e cells and their p210bcr-abl-expressing factor-independent derivatives. STI571 was a more potent inhibitor of 3H-thymidine incorporation in p210bcr-abl-expressing cells than was AG957, and it showed superior discrimination between inhibitory effects on parental cell lines and effects on their p210bcr-abl-expressing derivatives. Assays perfo..