TABLE 1.
Features of TKIs used in the experiments.
| TKI | Indication(s) | Primary target(s) | YES1 Kd (nM) | OCT1 IC50 (µM) | OCT1 inhibition | OCT2 inhibition |
|---|---|---|---|---|---|---|
| Dasatinib | CML, GIST | BCR/ABL, SRC | 0.3 | 0.56–1.09 | Yes | Yes |
| Gilteritinib | AML | FLT3, AXL | 445 | 0.01–0.02 | Yes | Yes |
| Ibrutinib | CLL, MCL | BTK | 27 | 0.89–1.18 | Yes | Yes |
| Lapatinib | Breast cancer | HER2, EGFR | >10,000 | — | No | No |
| Vandetanib | Thyroid cancer | EGFR, VEGFR | 120 | 1.35–9.05 | Yes | Yes |
CLL, chronic lymphocytic leukemia; CML, chronic myeloid leukemia; GIST, gastrointestinal stromal tumor; MCL, mantle cell lymphoma; AML, acute myeloid leukemia.