Figure 1. Chemical structure of 1R-Chl, imatinib, dasatinib, and their effects on BCR-ABL unmutated and mutated genes transduced into murine BM cells.

(A) 1R-Chl (left) targets the DNA sequences 5′-WGGWGW-3′. Bold, imidazole rings. imatinib (middle) targets Bcr-Abl kinase, and dasatinib (right) targets 14 out of 15 Bcr-Abl mutants. (B) Murine BM cells transduced with unmutated BCR-ABL and single point mutation Y253H, E255K, and T315I genes were tested for the effectiveness of 1R-Chl (125 nM to 1000 nM), 1S-Chl (500 nM and 1000 nM), imatinib (500 nM and 5000 nM; IC₅₀ = 260 nM for the native BCR-ABL transduced cells) [6], and dasatinib (10 nM and 100 nM; IC₅₀ = 0.8 nM for the native BCR-ABL transduced cells) [6]. Triplicate experiments were done, and the numbers of colonies were quantified 7 days after initial plating.