The c-RET proto-oncogene, which was originally identified as a transforming gene by transfection of T-cell lymphoma DNA into NIH3T3 cells, is a member of the receptor tyrosine kinase (RTK) gene superfamily that encodes a receptor tyrosine kinase involved in the regulation of glial cell line-derived neurotrophic factor (GDNF) signaling. Signaling proteins, such as Grb7/Grb10, PLCγ, Shc/Enigma and Grb2, are recruited by activated c-RET protein through binding to the phosphorylated tyrosine residues in c-RET protein’s COOH-terminal sequence, Y905, Y1015, Y1062 and Y1096 respectively. Moreover, results of in vivo studies suggest mutations of c-RET have been implicated in tumorigenesis, in which c-RET mRNA and/or protein have been found in tumors of neuroectodermal origin as well as in human neuroblastoma cell lines.
- RPI-1Catalog No. :C4239ATP-dependent RET kinase inhibitor
- AD57 (hydrochloride)Catalog No. :C3080polypharmacological cancer therapeutic that inhibits RET.
- RegorafenibCatalog No. :A8236Inhibitor of VEGFR/PDGFR/FGFR/mutant kit/RET/Raf-1
Regorafenib (BAY 73-4506) is a novel and orally active multikinase inhibitor of receptor tyrosine kinases VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET, Raf-1, B-RAF and B-RAFV600E with IC50 values of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM, 2.5 nM, 28 nM and 19 nM .
- SU5416Catalog No. :A3847VEGF receptor inhibitor and AHR agonist
SU5416 was found to inhibit VEGF-dependent phosphorylation of the Flk-1 receptor in Flk-1-overexpressing NIH 3T3 cells with an IC50 of 1.04±0.53 mM .
- Regorafenib monohydrateCatalog No. :A3751Tyrosine kinase inhibitorRegorafenib monohydrate is a multitargetedinhibitor of tyrosine kinase with IC50 values of 13nM, 4.2nM, 46nM, 2.5nM, 28nM, 19nM, 202nM, 22nM, 7nM, 1.5nM and 311nM, respectively for VEGFR-1, mVEGFR-2, mVEGFR-3, Raf-1, BRAF WT, BRAFV600E, FGFR-1, PDGFR-β, c-KIT, RETand TIE2 .
- Regorafenib hydrochlorideCatalog No. :A3750Tyrosine kinase inhibitorRegorafenib hydrochloride
- Amuvatinib (MP-470, HPK 56)Catalog No. :A4237Tyrosine kinase inhibitorAmuvatinib (also known as MP-470 or HPK 56), a synthetic carbothioamide, is a novel and potent tyrosine kinase inhibitor, which exerts in vitro and in vivo activities against multiple targets including mutant KIT, platelet-derived growth factor receptor alpha (PDGFRα) and DNA repair.
- Danusertib (PHA-739358)Catalog No. :A4116Pan-aurora kinase inhibitor
Danusertib (previously known as PHA-739358), a 3-aminopyrazole derivative identified during the development of the pyrrolopyrazole sub-series, is a potent small-molecule inhibitor of aurora kinases family members with a dominant inhibition for aurora B kinase (ABK).
- TG101209Catalog No. :A4145JAK2/3 inhibitorTG101209, a small-molecule identified by structure based design, is a selective inhibitor of janus kinase 2 (Jak2) that potently inhibits Jak/Stat pathway in multiple myeloma (MM) cell lines, such as cell harboring JAK2V617F or MPLW515L/K mutations which are commonly associated with polycythemia vera (PV) and primary myelofibrosis (PMF) respectively.