Kinase target profile of inhibitors that can be used for the treatment of chronic myeloid leukemia (CML).
TKI . | ABL . | ABLT315I . | Kit . | PDGFR . | SRC . | Aurora . | Others . |
---|---|---|---|---|---|---|---|
+, weak/moderate inhibition; ++, moderate/strong inhibition; +++, very strong inhibition. | |||||||
Abbreviations: TKI, tyrosine kinase inhibitor; NR, not reported; LCK, lymphocyte-specific protein tyrosine kinase; LYN, Lck/Yes-related novel tyrosine kinase. | |||||||
Imatinib | + | - | ++ | ++ | LCK | - | + |
Nilotinib | ++ | - | + | + | - | - | - |
Dasatinib | +++ | - | ++ | ++ | +++ | - | +++ |
Bosutinib | ++ | - | - | - | +++ | - | + |
INNO-406 | ++ | - | - | ++ | LYN | - | NR |
MK-0457 | + | + | - | - | - | +++ | NR |
XL228 | +++ | +++ | NR | NR | NR | +++ | NR |
PHA-739358 | ++ | ++ | + | NR | + | +++ | + |
AP24534 | +++ | +++ | NR | NR | NR | NR | NR |
SGX393 | +++ | +++ | - | - | LCK | - | + |
DC-2036 | +++ | +++ | NR | NR | ++ | NR | NR |
TKI . | ABL . | ABLT315I . | Kit . | PDGFR . | SRC . | Aurora . | Others . |
---|---|---|---|---|---|---|---|
+, weak/moderate inhibition; ++, moderate/strong inhibition; +++, very strong inhibition. | |||||||
Abbreviations: TKI, tyrosine kinase inhibitor; NR, not reported; LCK, lymphocyte-specific protein tyrosine kinase; LYN, Lck/Yes-related novel tyrosine kinase. | |||||||
Imatinib | + | - | ++ | ++ | LCK | - | + |
Nilotinib | ++ | - | + | + | - | - | - |
Dasatinib | +++ | - | ++ | ++ | +++ | - | +++ |
Bosutinib | ++ | - | - | - | +++ | - | + |
INNO-406 | ++ | - | - | ++ | LYN | - | NR |
MK-0457 | + | + | - | - | - | +++ | NR |
XL228 | +++ | +++ | NR | NR | NR | +++ | NR |
PHA-739358 | ++ | ++ | + | NR | + | +++ | + |
AP24534 | +++ | +++ | NR | NR | NR | NR | NR |
SGX393 | +++ | +++ | - | - | LCK | - | + |
DC-2036 | +++ | +++ | NR | NR | ++ | NR | NR |