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 (29):

Cat. No. Product Name Effect Purity
  • HY-10981
    Lenvatinib Inhibitor 99.87%
    Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
  • HY-10331
    Regorafenib Inhibitor ≥99.0%
    Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.
  • HY-112301
    Pralsetinib Inhibitor 99.56%
    Pralsetinib (BLU-667) is a highly potent, selective RET inhibitor. Pralsetinib (BLU-667) inhibits WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion with IC50s of 0.4, 0.3, 0.4, 0.4, and 0.4 nM, respectively.
  • HY-114370
    Selpercatinib Inhibitor 99.87%
    Selpercatinib (LOXO-292) is a RET kinase inhibitor extracted from patent WO2018071447A1, Compound Example 163, has an IC50 of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M) , and RET (G810R), respectively. Antineoplastic activity.
  • HY-10206
    Amuvatinib Inhibitor 98.07%
    Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.
  • HY-133553
    RET-IN-3 Inhibitor
    RET-IN-3 (compound 34) is a selective RETV804M kinase inhibitor, with an IC50 of 19 nM.
  • 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 (KDR). Effective brain penetration.
  • HY-16018
    Ilorasertib Inhibitor ≥98.0%
    Ilorasertib (ABT-348) is a potent and ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A with IC50s of 1 nM, 7 nM, 120 nM, respectively. Ilorasertib also suppresses RET tyrosine kinase, PDGFRβ and Flt1 with IC50s of 7 nM, 3 nM and 32 nM, respectively.
  • HY-124401
    BT-13 Agonist ≥99.0%
    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.
  • HY-13308
    Regorafenib Hydrochloride Inhibitor ≥98.0%
    Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
  • HY-18840
    BBT594 Inhibitor 99.94%
    BBT594 is a potent receptor tyrosine kinase RET inhibitor, used for cancer treatment.
  • HY-10410
    TG101209 Inhibitor 99.72%
    TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM, appr 30-fold selective for JAK2 than JAK3, and sensitive to JAK2V617F and MPLW515L/K mutations.
  • HY-10981A
    Lenvatinib mesylate Inhibitor 99.86%
    Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
  • HY-10032
    PF 477736 Inhibitor 99.21%
    PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo.
  • HY-15002
    AST 487 Inhibitor 99.20%
    AST 487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM.
  • HY-100459
    GSK3179106 Inhibitor 99.40%
    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.
  • HY-16018A
    Ilorasertib hydrochloride Inhibitor 98.91%
    Ilorasertib (ABT-348 hydrochloride) is a potent and ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A with IC50s of 1 nM, 7 nM, 120 nM, respectively. Ilorasertib (ABT-348 hydrochloride) also suppresses RET tyrosine kinase, PDGFRβ and Flt1 with IC50s of 7 nM, 3 nM and 32 nM, respectively.
  • HY-10331A
    Regorafenib monohydrate Inhibitor 99.96%
    Regorafenib monohydrate (BAY 73-4506 monohydrate) is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
  • HY-101963
    AD80 Inhibitor 99.85%
    AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.
  • HY-110193
    SPP-86 Inhibitor ≥99.0%
    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.
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