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-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-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-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-164413
    CLM3
    Inhibitor
    CLM3, a pyrazolopyrimidine derivative, is a multiple tyrosine kinase inhibitor. CLM3 shows antiproliferative and proapoptotic activity on endothelial and cancer cells, synergistically enhanced by SN38 (HY-13704). These effects are mainly due to its inhibition of phosphorylation of VEGFR-2, EGFR and RET tyrosine kinases and their related signaling pathways.
    CLM3
  • 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
  • HY-10981S1
    Lenvatinib-d5
    Inhibitor
    Lenvatinib-d5 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>5</sub>
  • HY-10981S2
    Lenvatinib-15N,d4
    Inhibitor
    Lenvatinib-15N,d4 is 15N and deuterated labeled Lenvatinib (HY-10981). 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-<sup>15</sup>N,d<sub>4</sub>
  • HY-145024
    RET-IN-6
    Inhibitor
    RET-IN-6 is a potent RET (rearranged during transfection) inhibitor with an IC50 of 4.57 nM (CN113461670A, compound 321).
    RET-IN-6
  • HY-P10044
    IGF1Rtide
    IGF1Rtide can be used as a RET kinase substrate for RET kinase assays.
    IGF1Rtide
  • HY-117873
    KBP-7018
    Inhibitor
    KBP-7018 is a tyrosine kinase-selective inhibitor. KBP-7018 has potent inhibitory effects on c-KIT, PDGFR, and RET with IC50 values of 10 nM, 7.6 nM and 25 nM, respectively. KBP-7018 can be used for the research of idiopathic pulmonary fibrosis.
    KBP-7018
  • HY-149539
    PLM-101
    Inhibitor
    PLM-101 is an orally available anticancer agent targeting FLT3 and RET with inhibitory activity against acute myeloid leukemia cells. PLM-101 inhibits RET, thereby inducing autophagic degradation of FLT3; and it inhibits the PI3K and Ras/ERK pathways, resulting in anti-leukemia activity. PLM-101 has anti-tumor efficacy in a mouse MV4-11 flank xenograft model (dose: 3, 10 mg/kg; po) and an allogeneic xenograft mouse model (dose: 40 mg/kg; po).
    PLM-101
  • HY-170809
    RET-IN-29
    Inhibitor
    RET-IN-29 (Compound 8W) is a selective RET kinase inhibitor. RET-IN-29 exhibits inhibitory potency against the BaF3 cells harboring CCDC6-RETV804M mutation with an IC50 value of 0.715 μM. RET-IN-29 is promising for research of non-small cell lung cancer (NSCLC).
    RET-IN-29
  • HY-151987
    RET-IN-20
    Inhibitor
    RET-IN-20 is a potent RET inhibitor with an IC50 value of 13.7 nM. RET-IN-20 decreases the expression of p-Ret, p-Shc protein. RET-IN-20 induces apoptosis. RET-IN-20 shows antiproliferative and anti-tumor activity.
    RET-IN-20
  • HY-146710
    RET-IN-16
    Inhibitor
    RET-IN-16 is a potent and selective RET inhibitor with IC50s of 3.98 nM, 8.42 nM, 15.05 nM, 7.86 nM, 5.43 nM and 8.86 nM for RET(WT), RET(M918T), RET(V804L), RET(V804M), RET-CCDC6 and RET-KIF5B, respectively. RET-IN-16 has anticancer effects.
    RET-IN-16
  • HY-153941
    RET-IN-24
    Inhibitor
    RET-IN-24 (Compound 26) is a selective RET tyrosine kinase inhibitor with antitumor activity.
    RET-IN-24
  • HY-112950
    RET-IN-1
    Inhibitor
    RET-IN-1 is a RET kinase inhibitor extracted from patent WO2018071447A1, Compound Example 552, has IC50s of 1 nM, 7 nM, and 101 nM for RET (WT), RET (V804M) , and RET (G810R), respectively .
    RET-IN-1
  • HY-153676
    RET-IN-23
    Inhibitor
    RET-IN-23 (compound 17) is a potent and orally active RET inhibitor with IC50 values of 1.32, 2.50, 6.54, 1.03, 1.47 nM for RET-WT, RET-CCDC6, RET-V804L, RET-V804M, RET-M918T, respectively. RET-IN-23 shows anti-tumor activity.
    RET-IN-23
  • HY-161775
    RET/TRKA-IN-1
    Inhibitor
    RET/TRKA-IN-1 (Compound 13) is a dual inhibitor for RET (IC50=0.375 µM) and TRKA. RET/TRKA-IN-1 inhibits cell viability of LC-2 and KM12, with GI50 of 0.72 and 0.25 μM. RET/TRKA-IN-1 arrests the cell cycle at G1 phase.
    RET/TRKA-IN-1
  • HY-156113
    RET-IN-25
    Inhibitor
    RET-IN-25 (compound 6b) is a RET kinase inhibitor with anticancer activity. RET-IN-25 inhibits medullary thyroid carcinoma (MTC) with IC50s of 3.6 μM (3 days) and 3.0 μM (6 days) against TT(C634R) MTC.
    RET-IN-25