1. Signaling Pathways
  2. Protein Tyrosine Kinase/RTK
  3. RET

RET

RET (REarranged during Transfection) is a transmembrane receptor tyrosine kinase that is activated by a complex consisting of a soluble glial cell line-derived neurotrophic factor (GDNF) family ligand (GFL) and a glycosyl phosphatidylinositol-anchored co-receptor, GDNF family receptors alpha (GFRalpha).

RET signalling is crucial for the development of the enteric nervous system. RET regulates the development of sympathetic, parasympathetic, motor, and sensory neurons, and is necessary for the postnatal maintenance of dopaminergic neurons. RET also plays a role as a driver oncogene in a variety of human cancers. Fusion of RET with several partner genes has been detected in papillary thyroid, lung, colorectal, pancreatic, and breast cancers, and tyrosine kinase inhibitors (TKIs) for RET (particularly RET-specific inhibitors) show promising effects against such cancers.

RET Related Products (106):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-133551
    WF-47-JS03
    Inhibitor 99.63%
    WF-47-JS03 is a potent and selective RET kinase inhibitor with IC50s of 1.7 nM and 5.3 nM for KIF5B-RET transfected Ba/F3 cells and CCDC6-RET transfected LC-2/ad lung cancer cells, respectively. WF-47-JS03 demonstrates >500-fold selectivity against kinase insert domain receptor (VEGFR2/KDR/Flk-1). Effective brain penetration.
    WF-47-JS03
  • HY-139590
    Zeteletinib
    Inhibitor 98.31%
    Zeteletinib (BOS-172738; DS-5010) is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2/KDR/Flk-1. 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.
    Zeteletinib
  • HY-110193
    SPP-86
    Inhibitor 99.62%
    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. SPP-86 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    SPP-86
  • HY-U00437
    Pz-1
    Inhibitor 99.90%
    Pz-1 is a potent RET and VEGFR2/KDR/Flk-1 inhibitor with IC50s of less than 1 nM for both wild type kinases.
    Pz-1
  • HY-136534
    RET V804M-IN-1
    Inhibitor 98.22%
    RET V804M-IN-1 (compound 5) is a wt-RET -selective inhibitors of RETV804M kinase, with an IC50 of 20 nM.
    RET V804M-IN-1
  • HY-145565
    Enbezotinib
    Inhibitor 99.50%
    Enbezotinib, an inhibitor of RET, can inhibit the RET autophosphorylation. Enbezotinib can be used for the research of cancer.
    Enbezotinib
  • HY-153175
    BT44
    Activator 99.08%
    BT44 is a selective RET activator. BT44 can penetrate through the blood-brain barrier and can be used for the research of neurodegenerative disorders and diabetes mellitus.
    BT44
  • HY-15769
    WHI-P180
    Inhibitor 99.84%
    WHI-P180 (Janex 3) is a multi-kinase inhibitor; inhibits RET, VEGFR2/KDR/Flk-1 and EGFR with IC50s of 5 nM, 66 nM and 4 μM, respectively.
    WHI-P180
  • HY-101246
    RPI-1
    Inhibitor 99.29%
    RPI-1 is a specific, orally available 2-indolinone Ret tyrosine kinase inhibitor. RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT in human medullary thyroid carcinoma TT cells. Antitumor activity.
    RPI-1
  • HY-112301A
    trans-Pralsetinib
    Inhibitor
    trans-Pralsetinib (trans-BLU-667) is a rearranged during transfection (RET) inhibitor extracted from patent US20170121312A1, Compound Example 129.
    trans-Pralsetinib
  • HY-18507
    AD57
    Inhibitor 98.08%
    AD57 is an orally active multikinase inhibitor, inhibits RET, BRAF, S6K and Src, with greatly reduces mTOR activity.
    AD57
  • HY-13342AS
    Apatinib-d8 free base
    Apatinib-d8 (free base) is the deuterium labeled Apatinib free base[1]. Apatinib free base (YN968D1 free base) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 (IC50=1 nM). Apatinib free base (YN968D1 free base) is an anti-angiogenic drug for the research of advanced or metastatic gastric cancer. Apatinib free base (YN968D1 free base) potently inhibits Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. It also inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ[2][3][4].
    Apatinib-d<sub>8</sub> free base
  • HY-10981S
    Lenvatinib-d4
    Inhibitor 99.59%
    Lenvatinib-d4 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities[1][2].
    Lenvatinib-d<sub>4</sub>
  • HY-133553
    RET-IN-3
    Inhibitor 99.51%
    RET-IN-3 (compound 34) is a selective RETV804M kinase inhibitor, with an IC50 of 19 nM.
    RET-IN-3
  • HY-10331S
    Regorafenib-d3
    Inhibitor ≥98.0%
    Regorafenib-d3 is a deuterium labeled Regorafenib. Regorafenib is a multi-targeted receptor tyrosine kinase inhibitor[1].
    Regorafenib-d<sub>3</sub>
  • HY-18317
    JNJ-38158471
    Inhibitor
    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.
    JNJ-38158471
  • HY-116116
    Tafetinib
    Inhibitor
    Tafetinib (SIM010603) is an oral multi-targets receptor tyrosine kinases inhibitor. Tafetinib inhibitsstem cell factor receptor (Kit),vascular endothelial growth factor receptor-2 (VEGFR-2),platelet-derived growth factor receptor-β (PDGFR-β),glial cell line-derived neurotrophic factor receptor (Rearranged during Transfection; RET), andFms-like tyrosine kinase-3 (FLT3)withIC50values between 5.0 and 68.1 nmol/l. Tafetinib inhibits the phosphorylation ofPDGFR-βandVEGFR-2. Tafetinib inhibits endothelial cell proliferation, endothelial cells chemotaxis, and corneal angiogenesis.
    Tafetinib
  • HY-34595
    Pyrazoloadenine
    Inhibitor 99.98%
    Pyrazoloadenine is a potent RET (REarranged during Transfection) lung cancer oncoprotein inhibitor. Pyrazoloadenine shows anticancer activity.
    Pyrazoloadenine
  • HY-10981R
    Lenvatinib (Standard)
    Inhibitor
    Lenvatinib (Standard) is the analytical standard of Lenvatinib. This product is intended for research and analytical applications. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
    Lenvatinib (Standard)
  • HY-162565
    CDD-2807
    Inhibitor
    CDD-2807 is an inhibitor for serine/threonine kinase 33 (STK33) with IC50 of 9.2 nM. CDD-2807 exhibits no significant toxicity in mice and can cross the blood-testis barrier without accumulating in the brain. CDD-2807 induces a reversible contraceptive effect and has potential for the development of the male contraceptive.
    CDD-2807