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Results for "

RET (G810R)

" in MedChemExpress (MCE) Product Catalog:

11

Inhibitors & Agonists

2

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. 상품명 Target 연구분야 Chemical Structure
  • HY-114370
    Selpercatinib
    10+ Cited Publications

    LOXO-292

    		 RET Cancer
    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 .
    Selpercatinib
  • HY-E70769
    RET G810R Recombinant Human Active Protein Kinase

    		RET Cancer
    Rearranged during transfection (RET) is a transmembrane receptor protein tyrosine kinase (PTK) activated normally by forming ternary complexes with its cognate ligands and co-receptors. RET alterations by point mutations and gene fusions were found in diverse cancers. RET G810R is a mutant of RET. RET G810R Recombinant Human Active Protein Kinase is a recombinant RET G810R protein that can be used to study RET G810R-related functions .
    RET G810R Recombinant Human Active Protein Kinase
  • HY-114370R
    Selpercatinib (Standard)

    LOXO-292 (Standard)

    		 Reference Standards RET Cancer
    Selpercatinib (Standard) is the analytical standard of Selpercatinib. This product is intended for research and analytical applications. 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 .
    Selpercatinib (Standard)
  • HY-176937
    HSN608

    		RET Apoptosis Cancer
    HSN608 is an orally active, potent RET G810 mutant inhibitor. HSN608 inhibits G810C, G810R, G810D. HSN608 induces Apoptosis. HSN608 inhibits the Selpercatinib (HY-114370)-resistant RET(G810C) CDX tumors .
    HSN608
  • HY-178964
    PROTAC RET Degrader 1

    		PROTACs RET Cancer
    PROTAC RET Degrader 1 (Compound 20) is an orally active and blood-brain barrier-crossing RET PROTAC degrader with DC50 values for RET (WT), RET (G810S), RET (G810C), and RET (G810R) of 1.7, 3, 12, and 21 nM, respectively. PROTAC RET Degrader 1 exhibits potent anti-proliferative activity in cancer cell lines carrying oncogenic RET fusions (such as KIF5B-RET, CCDC6-RET) or mutations (such as RET (C634W)). PROTAC RET Degrader 1 shows significant anti-tumor activity in human tumor xenograft (PDX) mouse models. PROTAC RET Degrader 1 can be used for the study of RET-positive cancers Pink: RET ligand (HY-179308); Blue: CRBN ligand (HY-179307); Black: Linker) .
    PROTAC RET Degrader 1
  • HY-112950
    RET-IN-1

    		RET Cancer
    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-144170
    RET-IN-14

    		RET Btk Cancer
    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-W759629
    Selpercatinib-d3

    LOXO-292-d3

    		 Isotope-Labeled Compounds RET Cancer
    Selpercatinib-d3 (LOXO-292-d3) is deuterium labeled Selpercatinib. 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 .
    Selpercatinib-d3
  • HY-114370S
    Selpercatinib-13C,d3

    LOXO-292-13C,d3

    		 Isotope-Labeled Compounds Cancer
    Selpercatinib- 13C,d3 (LOXO-292- 13C,d3) is 13C labeled Selpercatinib. 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 .
    Selpercatinib-13C,d3
  • HY-170926
    CQ1373

    		RET Apoptosis Cancer
    CQ1373 is a potent RET inhibitor, demonstrating cellular potency with IC50 values of 13.0, 25.7 and 28.4 nM against BaF3 cells expressing CCDC6-RET, CCDC6-RET-G810C and CCDC6-RET-G810R, respectively. CQ1373 exhibits good selectivity toward wild-type RET and solvent front mutants G810C/R with IC50 values of 4.2, 7.1 and 32.4 nM, respectively. CQ1373 inhibits RET phosphorylation and downstream signaling through SHC. CQ1373 induces Apoptosis and cell cycle arrest in BaF3 cells. CQ1373 exhibits anti-tumor efficacy and can be used for cancer research .
    CQ1373
  • HY-183684
    RET-IN-33

    		RET VEGFR PDGFR Akt ERK Endocrinology Cancer
    RET-IN-33 is a moderately selective inhibitor of RET mutants. RET-IN-33 potently inhibits G810 mutants, with IC50 values of 4.43 nM (G810R), 3.28 nM (G810C) and 0.51 nM (G810S), respectively. RET-IN-33 also inhibits other RET mutants: V804M (IC50 0.73 nM), V804L (IC50 0.36 nM), Y806H (IC50 0.74 nM) and M918T (IC50 0.55 nM). RET-IN-33 also inhibits other kinases, with an IC50 of 1.50 nM against VEGFR2 and 1.60 nM against PDGFRα. RET-IN-33 blocks the autophosphorylation of RET mutants and the downstream SHC/AKT/ERK signaling pathway. RET-IN-33 selectively inhibits the proliferation of RET-driven cell models without affecting non-RET-dependent or normal cells. RET-IN-33 exhibits dose-dependent antitumor efficacy in RET-driven xenograft models. RET-IN-33 can be used for the research of medullary thyroid carcinoma, papillary thyroid carcinoma and non-small cell lung cancer .
    RET-IN-33

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