GSK3179106 is a potent, selective and gut-restricted RET kinase inhibitor with IC50 value of 0.4nM.

Blu667 is a highly potent and selective RET inhibitor with IC50 value of 0.4nM.

Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research.

Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13/4.2/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.

AD80 is a multikinase inhibitor with inhibitions on RET, RAF, SRC and S6K.

TG 101348 is an inhibitor of JAK2 with an IC₅₀ of 6 nM and also inhibits related kinases FLT3, RET, and JAK3 with less potent activity, having IC₅₀ values of 25, 17 and 169 nM, respectively.

JNJ-38158471 is a well tolerated, orally available, highly selective VEGFR-2 inhibitor, with an IC50 of 40 nM. JNJ-38158471 also inhibits Ret and Kit with IC50s of 180 and 500 nM, respectively .

AST-487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM. AST487 also inhibits RET,KDR,c-KIT,and c-ABL kinase with IC50 values below 1 μM.

CEP-32496 is an inhibitor of BRAF V600E (IC50 = 14 nM), WT (IC50 = 34 nM) and c-Raf (IC50 = 39 nM). It also exhibits certain inhibitory activity against Abl-1, c-Kit, Ret, PDGFRβ and VEGFR2.

Danusertib is a pyrrolo-pyrazole and small molecule Aurora kinases inhibitor with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively. It is modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc.

BBT594 is a potentreceptor tyrosine kinase RET inhibitor, used for cancer treatment.

SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase( IC50 :8 nM). SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells.