Table 2.

BCR/ABL mutations detectable in CML patients treated with imatinib

Mutant	IC50* imatinib	may benefit from IM-dose-escalation**	IC50* dasatinib	IC50* nilotinib
no (wt)	250–500	-	0.8	13
M244V	1,600–3,100	yes	1.3	38
M244I	1,400	yes	nk	nk
G250E	>1,000 (>3,000)	no	1.8	48
Q252H	1,300–2,900	yes	3.4	70
Y253H	4,000–17,000	no	1.3	450
Y253F	1,800–5,000	no	1.4	125
E255K	5,000–12,000	no	5.6	200
E255V	6,000–20,000	no	11	430
F311L	480–1,300	no	1.3	23
T315I	>10,000	no	>200	>2,000
F317L	1,000–2,300	no	7.4	50
M351T	900–4,900	yes	1.1	15
M351I	1,600	yes	nk	nk
F359V	1,400–1,800	yes	2.2	175
E355G	2,000–2,400	yes	nk	nk
V379I	1,000–1,600	yes	0.8	51
L387M	1,000–1,100	yes	2	49
H396P	850–4,300	no	0.6	41
H396R	1,750–5,400	no	1.3	41

Notes:

^*IC50 values are given in nM and refer to published data obtained with Ba/F3 cells exhibiting wild type BCR/ABL or various BCR/ABL mutants using cell – proliferation assays (O’Hare et al 2005; Martinelli et al 2005);

^**recommendations are derived from Martinelli and colleagues (2005).

Abbreviations: IM, imatinib; wt, wild type; nk, not known.