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c-RET

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.

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  1. RPI-1
    Catalog No. :
    C4239
    ATP-dependent RET kinase inhibitor
  2. AD57 (hydrochloride)
    Catalog No. :
    C3080
    polypharmacological cancer therapeutic that inhibits RET.
  3. Regorafenib
    Catalog No. :
    A8236
    Inhibitor 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 [1].

  4. SU5416
    Catalog No. :
    A3847
    VEGF 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 .

  5. Regorafenib monohydrate
    Catalog No. :
    A3751
    Tyrosine kinase inhibitor
    Regorafenib 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 .
  6. Regorafenib hydrochloride
    Catalog No. :
    A3750
    Tyrosine kinase inhibitor
    Regorafenib hydrochloride
  7. Amuvatinib (MP-470, HPK 56)
    Catalog No. :
    A4237
    Tyrosine kinase inhibitor
    Amuvatinib (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.
  8. Danusertib (PHA-739358)
    Catalog No. :
    A4116
    Pan-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).

  9. TG101209
    Catalog No. :
    A4145
    JAK2/3 inhibitor
    TG101209, 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.

9 Items

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