Table 3. Anti-tumor activities of SFK inhibitors.
Drug | Examples of targets | Activities on tumor cells | Clinical trials | |||
---|---|---|---|---|---|---|
Proliferation | Apoptosis | Invasion, Metastasis | Drug re-sensitivity | |||
Bosutinib | SFKs, ABL, CAMK2G, TEC, STE20 | Reduced [166, 167] | Increased [168] | Reduced [169, 170] | Restored [171] | CML [172] and breast cancer [173] |
Dasatinib | SFKs, BCR/ABL, c-Kit, Ephrins, RTKs | Reduced [174–177] | Increased [178–180] | Reduced [181, 182] | Restored [123, 134] | Prostate [183] and breast [184, 185] cancer |
Saracatinib | SFKs, BCR/ABL, EGFR | Reduced [186, 187] | Increased [132] | Reduced [188, 189] | Restored [190, 191] | Melanoma [192] and lung [193] cancer |
PP2 | SFKs, RIP2, CK1δ | Reduced [194] | Increased [195] | Reduced [196] | Restored [197] | Not tested |
A-419259 | SFKs | Reduced [118, 198] | Increased [118] | Reduced [198] | Not tested | Not tested |
RK-20449 | HCK | Reduced [142] | Increased [142] | Not tested | Not tested | Not tested |
SU6656 | SFKs, PGDF, BRSK2, AMPK, Aurora C, Aurora B, CaMKKβ | Reduced [199] | Increased [200] | Reduced [201] | Restored [66] | Not tested |