Table 2.
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.