Table 1 Kinase inhibitors with inhibitory activity towards RET

PP1

Lyc (5nM), fyn (6 nM), Src (170 nM), Csk (520 nM), CK1δ (1060 nM), p38MAPK (640 nM), RET (80 nM)

[20, 26, 27]

RPI-1

MET (7.5 μM), RET (170 nM),

[28–30]

PHA-739358 (Danusertib)

Aurora kinase A/B/C (13 nM/79 nM/61 nM), BCR-ABL (25 nM), RET(31 nM), FGFR1 (47 nM)

[31]

TG101209

JAK2 (6 nM), FLT3 (25 nM), RET (17 nM)

[32]

SU 5416 (Semaxanib)

RET (944 nM), VEGFR (nM), KIT, MET, FLT3

[33, 34]

SU11248 (Sunitinib)

RET (224 nM), VEGFR2 (4 nM), FLT3 (8–14 nM), KIT (1–10 nM), PDGFRβ (39 nM), CSF1R (50–100 nM)

[35]

XL184 (Cabozantinib)

VEGFR2 (0.035 nM), MET (1.3 nM), RET (4 nM), KIT (4.6 nM), FLT-1/3/4 (12 nM/ 11.3 nM /6 nM, 14.3 nM), TIE2 (14.3 nM), AXL (7 nM)

[36]

BAY 43–9006 (Sorafenib)

RET (5.9- 47 nM), BRAF (25 nM), VEGFR1/2/3 (20–90 nM), FLT3 (33 nM), p38MAPK (38 nM), PDGFRβ (57 nM), KIT (68 nM)

[35, 37]

ZD6474 (Vandetanib)

RET (130 nM), VEGFR2 (40 nM), VEGFR3 (110 nM), EGFR (500 nM)

[38, 39]

AP24534 (Ponatinib)

RET (7 nM), ABL (0.4 nM), Lyn (0.2 nM), FLT3 (13 nM), KIT (13 nM), FGFR1 (2 nM), PDGFRα (1 nM), Src (5.4 nM), VEGFR2 (2 nM)

[40, 41]

NVP-AST487

RET (880 nM), KDR (170 nM), FLT-4 (790 nM), KIT (500 nM), FLT-3 (520 nM), ABL (20 nM)

[42]

NVP-BBT594

RET (~100 nM), JAK2 (1 nM), Tyk2 (1 nM), JAK3 (5 nM), JAK1 (15 nM), FAK (100 nM), IRK-3P (200 nM), ZAP70 (200 nM), FGFR2 (940 nM)

[43, 44]