c-Ret

Regorafenib (BAY 73-4506) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf. Regorafenib (BAY 73-4506) is an orally bioavailable multikinase inhibitor targeting both the tumor and its vasculature.

Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2

TG101209, a novel JAK2 inhibitor, has significant in vitro activity in multiple myeloma and displays preferential cytotoxicity for CD45+ myeloma cells.

Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.

RPI-1 is a competitive, potent ATP-dependent Ret kinase inhibitor.

Regorafenib is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.

AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.

Pralsetinib (BLU-667) is a highly potent, selective RET inhibitor.

SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC50 of 8 nM.

GSK3179106 is a potent and selective RET kinase inhibitor with an IC50 of 0.4 nM.

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

Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret.

cis-Pralsetinib (cis-BLU-667) is a highly potent and selective inhibitor of rearranged during transfection (RET), with IC50s ranging from 0.3 to 0.4 nM for WT RET and four enzyme variants (V804L, V804M, M918T, CCDC6-RET), and with broad, robust and anti-tumor activity against multiple RET-driven solid tumor types.