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 (74):

Cat. No. Product Name Effect Purity Chemical Structure
  • 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-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-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-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-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
  • HY-149413
    FHND5071
    Inhibitor
    FHND5071 is a potent and selective RET kinase inhibitor, FHND5071 can exert antitumor effects by inhibiting RET autophosphorylation. FHND5071 can be used for tumor diseases research.
    FHND5071
  • HY-14979A
    ML786 dihydrochloride
    Inhibitor
    ML786 dihydrochloride is a potent and orally bioavailable Raf inhibitor, with IC50s of 2.1, 4.2, and 2.5 nM for V600EΔB-Raf, wt B-Raf, and C-Raf, respectively. ML786 dihydrochloride also inhibits Abl-1, DDR2, EPHA2, VEGFR2/KDR/Flk-1, and RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 dihydrochloride can be used for the research of cancers.
    ML786 dihydrochloride
  • HY-143546
    RET-IN-9
    Inhibitor
    RET-IN-9 is a potent inhibitor of RET. RET kinase is a single-pass transmembrane receptor tyrosine kinase that plays an important role in the development of the kidney and enteric nervous system, and the maintenance of homeostasis in the nervous, endocrine, hematopoietic, and male reproductive systems. RET-IN-9 has the potential for the research of RET-related disease including non-small cell lung cancer and medullary thyroid cancer (extracted from patent WO2021115457A1, compound 29).
    RET-IN-9
  • HY-151377
    RET-IN-19
    Inhibitor
    RET-IN-19 (compound 59) is a potent RET inhibitor, with IC50 values of 6.8 and 13.51 nM against RET-wt and RET V804M, respectively. RET-IN-19 shows anticancer activity. RET-IN-19 can be used for non-small cell lung cancer (NSCLC) research.
    RET-IN-19
  • HY-156471
    RET-IN-26
    Inhibitor
    RET-IN-26 (compound D5) is RET kinase inhibitor, with the IC50 of 0.33 μM.
    RET-IN-26
  • HY-146680
    FLT3/ITD-IN-4
    Inhibitor
    FLT3/ITD-IN-4 (Compound 16) is a selective FMS-like tyrosine kinase 3 internal tandem duplications (FLT3-ITD) inhibitor with an IC50 of 2.3 nM. FLT3/ITD-IN-4 can be used for acute myeloid leukemia research.
    FLT3/ITD-IN-4
  • HY-144170
    RET-IN-14
    Inhibitor
    RET-IN-14 (compound 49) is a potent RET inhibitor with IC50s of <0.51 nM, 9.3 nM, 1.3 nM, 9.2 nM, 15 nM for RET (WT), RET (G810R), RET (V804M), BTK and BTK (C481S), respectively. RET-IN-14 has the potential for tumors research
    RET-IN-14
  • HY-120214
    TAS05567
    TAS05567 is a potent, highly selective, ATP-competitive and orally active Syk inhibitor with an IC50 of 0.37 nM. In a panel of 192 kinases, TAS05567 only shows >70% inhibition of Syk and 4 other kinases (FLT3, JAK2, VEGFR2/KDR/Flk-1 and RET with IC50s of 10 nM, 4.8 nM, 600 nM and 29 nM, respectively). TAS05567 can be used for humoral immune-mediated inflammatory conditions such as autoimmune and allergic diseases.
    TAS05567
  • HY-144029
    RET-IN-13
    Inhibitor
    RET-IN-13 (compound 1), a quinoline compound, is a potent RET inhibitor with IC50s of 0.5 nM, 0.9 nM for RET (WT) and RET (V804M), respectively. RET-IN-13 has the potential for tumors or intestinal diseases related to abnormal activation of RET research.
    RET-IN-13
  • HY-141896
    RET-IN-7
    Inhibitor 98.00%
    RET-IN-7 demonstrates potent in vitro RET kinase inhibition and robust in vivo efficacy in RET-driven tumor xenografts upon multiday dosing in mice.
    RET-IN-7
  • HY-147563
    RET-IN-17
    Inhibitor
    RET-IN-17 is a potent inhibitor of RET. RET-IN-17 has the potential for the research of pain associated with IBS and other gastrointestinal disorders and for the research of cancers with constitutive RET kinase activity (extracted from patent WO2016038552A1, compound 1).
    RET-IN-17