2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. RET
  5. RET Inhibitor

RET Inhibitor

RET Inhibitors (90):

Cat. No. Product Name Effect Purity
  • HY-10981
    Lenvatinib
    		Inhibitor 99.75%
    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 99.93%
    Regorafenib (BAY 73-4506) 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 shows very robust antitumor and antiangiogenic activity.
  • HY-114370
    Selpercatinib
    		Inhibitor 99.83%
    Selpercatinib (LOXO-292) is a potent, selective RET kinase inhibitor with IC50 values of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M), and RET (G810R), respectively. Selpercatinib has anticancer activity.
  • HY-112301
    Pralsetinib
    		Inhibitor 99.98%
    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-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-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.
  • HY-159824
    Soxataltinib
    		Inhibitor
    Soxataltinib (example 7) is a potent inhibitor of RET-kinase, with the IC50 of 0.601 nM. Soxataltinib plays an important role in cancer research.
  • 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.
  • HY-10331A
    Regorafenib monohydrate
    		Inhibitor 99.96%
    Regorafenib (BAY 73-4506) monohydrate 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 monohydrate shows very robust antitumor and antiangiogenic activity.
  • HY-13308
    Regorafenib Hydrochloride
    		Inhibitor 99.58%
    Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) is a multi-target inhibitor for VEGFR1/Flt-1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
  • HY-15002
    AST 487
    		Inhibitor 99.42%
    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-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/KDR/Flk-1, 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-10410
    TG101209
    		Inhibitor 99.22%
    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-10206
    Amuvatinib
    		Inhibitor 99.47%
    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-101963
    AD80
    		Inhibitor 99.88%
    AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.
  • HY-18840
    BBT594
    		Inhibitor 99.86%
    BBT594 is a potent receptor tyrosine kinase RET inhibitor, used for cancer treatment.
  • HY-132846
    Vepafestinib
    		Inhibitor 98.61%
    Vepafestinib (TAS0953/HM06; compound 6) is a RET inhibitor (extracted from patent WO2019039439). Vepafestinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • 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.
  • 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.
  • HY-156135
    NSC194598
    		Inhibitor ≥98.0%
    NSC194598 is a p53 DNA-binding inhibitor with IC50 value of 180 nM and 2-40 μM for in vitro and in vivo, respectively. NSC194598 interferes with transcriptional activation of mutated RET gene in human medullary thyroid carcinoma TT cells. NSC194598 can be used for acute toxicity to normal tissues by radiation and chemotherapy research.