Table 2.
Inhibitors of the Src-family and Syk.
| Compound |
Primary target(s) (IC50 in cell free assay) |
Other targets (IC50 in cell free assay) |
Clinical relevance |
|---|---|---|---|
| Dasatinib | Src (0.8 nM), Abl (<1 nM) | c-Kit (79 nM) | Approved in chronic myeloid leukemia and acute lymphoblastic leukemia (33) |
| Bosutinib (34) | Src (1.2 nM), Abl (1 nM) | n.a | Approved in chronic myeloid leukemia (35) |
| PP1 (36) | Lck (5 nM), Fyn (6 nM) | Hck (20 nM), Src (170 nM), Bcr-Abl (1 μM), Kit (75 nM), EGFR (250 nM) | – |
| PP2 (36) | Lck (4 nM), Fyn (5 nM), Hck (5 nM) | EGFR (480 nM), other 56 kinases at 10 μM (37) | – |
| Fostamatinib (38) | Syk (41 nM), Flt3 | 79 kinases <100 nM (39) | Approved in immune thrombocytopenia (40) |
| Entospletinib (41) | Syk (7.7 nM) | TNK1 (<100 nM) (39) | Investigated in hematological malignancies (42) |
| P505-15 (43) | Syk (1–2 nM) | Fgr (81 nM), Yes (123 nM), MLK1 (88 nM) | – |
| RO9021 (44) | Syk (5.6 nM) | n.a | – |
| PRT318 (45) | Syk (4 nM) | n.a | – |
| TAK-659 (46) | Syk (3.2 nM) | Flt3 (4.6 nM), ZAP-70 (75 nM), Jak3 (114 nM), VEGFR2 (135 nM) |
Investigated in hematological malignancies and solid tumors (47) |
Obtained from MedChemExpress and Selleckchem. n.a, not available.