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. 2006 Jun 13;108(7):2332–2338. doi: 10.1182/blood-2006-02-004580

Table 2.

Cellular proliferation IC50 values of BCR-ABL point mutants recovered in the presence of nilotinib and dasatinib

Nilotinib
Dasatinib
Imatinib mesylate
Mutation IC50, nM Fold change IC50, nM Fold change IC50, nM Fold change
L248V NR* NR* NR NR NR NR
G250E 48* 4* 1.8 2 1350 5
Q252H 70 4 3.4 2 1325 5
Y253H 450 35 1.3 2 > 6400 > 25
E255K 200* 14* 5.6 7 5200 20
E255V 430 33 11 14 > 6400 > 25
E292V NR* NR* NR NR NR NR
V299L NR NR 18* 13.4* 540 1.7
T3151 > 2000 > 154 > 200 > 250 > 6400 > 25
F317C NR NR NR* NR* 1200 3
F317L 50 4 7.4* 9* 1050 4
F3171 NR NR NR* NR* NR NR
F317V 350 1.1 53 40 500 1.3
F359C NR NR NR* NR* 1200 3

Imatinib mesylate values are provided for comparison.

NR indicates not reported.

*

Mutants recovered at lower drug concentrations.

Mutations recovered at intermediate drug concentrations.

Mutations recovered at high drug concentrations.18,21,28