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RET

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RET (REarranged during Transfection) is a receptor protein tyrosine kinase, which activates multiple signal transduction pathways. RET protein is composed of three domains: an extracellular ligand-binding domain, a transmembrane domain, and a cytoplasmic tyrosine kinase domain. The RET receptor tyrosine kinase (RTK) regulates key aspects of cellular proliferation and survival by regulating the activity of the mitogen- activated protein kinase (MAPK) and PI3K/Akt signaling pathways. RET also interacts directly with other kinases such as the epidermal growth factor receptor (EGFR) and hepatocyte growth factor receptor (MET) and the focal adhesion kinase (FAK). Furthermore, BRAF and p38MAPK are downstream targets of RET. Kinase inhibitors that simultaneously inhibit RET and its downstream targets.

RET tyrosine kinase receptor presents an attractive therapeutic target for the treatment of certain cancer subsets. Deregulated RET activity has been identified as a causative factor in the development, progression and response to therapy of thyroid carcinoma. Elevated RET expression has been associated with the development of endocrine resistance in human breast cancer.

Products Related to RET(32)

  • GC10035 structure
    GC10035TG101209
    CAS: 936091-14-4
    Purity: >99.50%

    An inhibitor of JAK2, FLT3, RET, and JAK3

  • GC10111 structure
    GC10111Regorafenib
    CAS: 755037-03-7
    Purity: >99.00%

    Regorafenib is an orally active multi-kinase inhibitor with IC 50 values of 13/4.2/46, 22, 7, 1.5 and 2.5nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.

  • GC10914 structure
    GC10914AST 487
    CAS: 630124-46-8
    Purity: >99.00%

    A multi-kinase inhibitor

  • GC14292 structure
    GC14292Apatinib Mesylate
    CAS: 811803-05-1
    Purity: >98.00%

    Apatinib Mesylate blocks the downstream signal transduction of VEGF pathway to inhibit neovascularization.

  • GC14534 structure
    GC14534Regorafenib monohydrate
    CAS: 1019206-88-2
    Purity: >99.50%

    A multi-kinase inhibitor

  • GC14606 structure
    GC14606Regorafenib hydrochloride
    CAS: 835621-07-3
    Purity: >99.50%

    A multi-kinase inhibitor

  • GC15454 structure
    GC15454Lenvatinib (E7080)
    CAS: 417716-92-8
    Purity: >99.50%

    E7080, known as lenvatinib, is an oral multitargeted tyrosine kinase inhibitor including VEGF, FGF and SCF receptors that has been shown to improve the survival rate of patients with radioiodine-refractory thyroid cancer.

  • GC16391 structure
    GC16391Amuvatinib (MP-470, HPK 56)
    CAS: 850879-09-3
    Purity: >98.00%

    A multi-targeted RTK inhibitor

  • GC18492 structure
    GC18492GSK3179106
    CAS: 1627856-64-7
    Purity: >99.00%

    A RET kinase inhibitor

  • GC19062 structure
    GC19062BBT594
    CAS: 882405-89-2
    Purity: >99.50%

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

  • GC31780 structure
    GC31780Pralsetinib (Blu667)
    CAS: 2097132-94-8
    Purity: >98.50%

    Pralsetinib (Blu667) is a selective inhibitor of the rearranged during transfection (RET) kinase, indicated for the treatment of certain RET-altered positive tumors.

  • GC32797 structure
    GC32797AD80
    CAS: 1384071-99-1
    Purity: >99.50%

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

  • GC33192 structure
    GC33192Selpercatinib
    CAS: 2152628-33-4
    Purity: >98%

    A RET kinase inhibitor

  • GC33362 structure
    GC33362Amuvatinib hydrochloride (MP470 hydrochloride)
    CAS: 1055986-67-8
    Purity: >98%

    Amuvatinib hydrochloride (MP470 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. Amuvatinib hydrochloride (MP470 hydrochloride) (MP470 hydrochloride) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.

  • GC34159 structure
    GC34159Ilorasertib (ABT-348)
    CAS: 1227939-82-3
    Purity: >98%

    Ilorasertib (ABT-348) (ABT-348) is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib (ABT-348) also is a potent VEGF, PDGF inhibitor. Ilorasertib (ABT-348) has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).

  • GC34509 structure
    GC34509BT-13
    CAS: 924537-98-4
    Purity: >99.50%

    BT-13 is a potent and selective glial cell line-derived neurotrophic factor (GDNF) receptor RET agonist independently of GFLs, promoting neurite growth from sensory neurons in vitro and attenuates experimental neuropathy in the Rat.

  • GC34809 structure
    GC34809SPP-86
    CAS: 1357349-91-7
    Purity: >99.50%

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

  • GC36438 structure
    GC36438Lenvatinib mesylate
    CAS: 857890-39-2
    Purity: >99.00%

    An inhibitor of VEGFR2 and VEGFR3

  • GC37047 structure
    GC37047Pz-1
    CAS: 1800505-64-9
    Purity: >99.00%

    Pz-1 is a potent RET and VEGFR2 inhibitor with IC50s of less than 1 nM for both wild type kinases.

  • GC37933 structure
    GC37933WHI-P180 hydrochloride
    CAS: 153437-55-9
    Purity: >98%

    WHI-P180 (Janex 3) is a multi-kinase inhibitor; inhibits RET, KDR and EGFR with IC50s of 5 nM, 66 nM and 4 μM, respectively.

  • GC38519 structure
    GC38519Ilorasertib hydrochloride
    CAS: 1847485-91-9
    Purity: >98.50%

    Ilorasertib (ABT-348) hydrochloride is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib hydrochloride also is a potent VEGF, PDGF inhibitor. Ilorasertib hydrochloride has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).

  • GC49686 structure
    GC49686N-desmethyl Regorafenib N-oxide
    CAS: 835621-12-0
    Purity: >90.00%

    An active metabolite of regorafenib

  • GC60592 structure
    GC60592APS6-45
    CAS: 2188236-41-9
    Purity: >99.50%

    APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity.

  • GC64340 structure
    GC64340Zeteletinib
    CAS: 2216753-97-6
    Purity: >98%

    Zeteletinib (BOS-172738; DS-5010) is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib shows exquisite potency for the wild type RET, RETV804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib has potent antitumor activity.