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 (92):

Cat. No. Product Name Effect Purity Chemical Structure
  • 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-100459
    GSK3179106
    Inhibitor 98.41%
    GSK3179106 is an orally active and selective RET kinase inhibitor with IC50s of 0.4 nM, 0.2 nM for human RET and rat RET, respectively. GSK3179106 has the potential for irritable bowel syndrome (IBS) through the attenuation of post-inflammatory and stress-induced visceral hypersensitivity.
    GSK3179106
  • 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-139590
    Zeteletinib
    Inhibitor 99.06%
    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-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-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-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-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-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-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-34595
    Pyrazoloadenine
    Inhibitor 99.98%
    Pyrazoloadenine is a potent RET (REarranged during Transfection) lung cancer oncoprotein inhibitor. Pyrazoloadenine shows anticancer activity.
    Pyrazoloadenine
  • HY-10331B
    Regorafenib mesylate
    Inhibitor
    Regorafenib (BAY 73-4506) mesylate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/Flt-1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib mesylate shows very robust antitumor and antiangiogenic activity.
    Regorafenib mesylate
  • HY-139590A
    Zeteletinib hemiadipate
    Inhibitor
    Zeteletinib (BOS-172738; DS-5010) hemiadipate is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2/KDR/Flk-1. Zeteletinib hemiadipate shows exquisite potency for the wild type RET, RETV804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib hemiadipate has potent antitumor activity.
    Zeteletinib hemiadipate
  • HY-132193
    RET-IN-4
    Inhibitor
    RET-IN-4 is a potent, selective and orally active RET inhibitor with IC50s of 1.29 nM, 1.97 nM, and 0.99 nM for RET (WT), RET (V804M), and RET (M918T), respectively. RET-IN-4 exhibits better kinases selectivity against JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). RET-IN-4 has anticancer effects.
    RET-IN-4
  • HY-10206A
    Amuvatinib hydrochloride
    Inhibitor
    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. Amuvatinib hydrochloride (MP470 hydrochloride) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.
    Amuvatinib hydrochloride
  • HY-144422
    RET-IN-15
    Inhibitor
    RET-IN-15 is a rearranged during transfection (RET) kinase inhibitor extracted from patent WO2021115457A1 compound 51. RET-IN-15 can be used for the research of cancer.
    RET-IN-15