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. Author manuscript; available in PMC: 2010 Mar 15.
Published in final edited form as: Cancer Res. 2009 Mar 10;69(6):2384–2392. doi: 10.1158/0008-5472.CAN-08-3953

Table 2.

Biochemical activities of the DSA compounds against clinically-relevant, imatinib-resistant Abl mutants and the corresponding c-Src mutants.

IC50 (nM)
Abl wt Abl Y253H Abl E255V Abl 359V Abl T315I* Src wt Src F278H Src E280V Src F382V Src T338I
DSA1 10 ± 3 25 ± 8 40 ± 5 27 ± 1 64 ± 5 4.6 ± 1.5 14 ± 2 6.5 ± 0.8 13 ± 5 6.4 ± 1.2
DSA2 14 ± 3 N/D N/D N/D 71 ± 3 4.6 ± 0.9 N/D N/D N/D 11 ± 2
DSA3 2.9 ± 0.5 N/D N/D N/D 11 ± 1 < 1 N/D N/D N/D 4.7 ± 1.0
DSA4 18 ± 3 N/D N/D N/D 45 ± 9 6.4 ± 2.2 N/D N/D N/D 15 ± 1
DSA5 7.2 ± 1.3 N/D N/D N/D 17 ± 3 3.4 ± 1.0 N/D N/D N/D 5.3 ± 1.0
DSA6 7.6 ± 1.4 N/D N/D N/D 45 ± 2 3.0 ± 0.6 N/D N/D N/D 9.6 ± 1.0
DSA7 1.5 ± 0.2 2.3 ± 0.2 3.8 ± 0.8 3.7 ± 0.4 6.3 ± 0.7 < 1 1.7 ± 0.1 1.3 ± 0.4 2.1 ± 0.7 2.6 ± 0.5
DSA8 2.7 ± 0.5 3.5 ± 0.1 9.5 ± 3.8 3.8 ± 0.8 33 ± 3 2.8 ± 0.3 7.0 ± 2.0 4.0 ± 1.2 4.4 ± 1.7 18 ± 6
DSA9 7.7 ± 5.3 N/D N/D N/D 92 ± 35 8.3 ± 4.2 N/D N/D N/D 13 ± 5
imatinib 11 ± 3 310 ± 30 76 ± 10 32 ± 2 >10000 >10000 >10000 >10000 >10000 >10000
*

Full length Abl Thr315Ile was obtained from a commercial source (Invitrogen) whereas the other proteins are kinase domain constructs expressed and purified from bacteria. N/D = not determined. All activity assays were performed in triplicate or quadruplicate.