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Results for "

RET-G810

" in MedChemExpress (MCE) Product Catalog:

13

Inhibitors & Agonists

2

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-114370
    Selpercatinib
    5+ 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-E70768
    RET G810C 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 G810C is a mutant of RET. RET G810C Recombinant Human Active Protein Kinase is a recombinant RET G810C protein that can be used to study RET G810C-related functions .
    RET G810C Recombinant Human Active Protein Kinase
  • 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-E70770
    RET G810S 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 G810S is a mutant of RET. RET G810S Recombinant Human Active Protein Kinase is a recombinant RET G810S protein that can be used to study RET G810S-related functions .
    RET G810S Recombinant Human Active Protein Kinase
  • 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-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-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-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-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-168867
    RD-23

    		PROTACs RET Apoptosis Cancer
    RD-23 is an orally active and selective RET PROTAC degrader. RD-23 promotes ubiquitination and degradation of RET G810C mutation, with a DC50 value of 11.7 nM. RD-23 inhibits the activation of downstream Shc signaling and induces Apoptosis. RD-23 can be used for the research of RET-related cancers (Pink: RET ligand-2 (HY-168868); Blue: E3 ligase CRBN ligand; Black: linker) .
    RD-23
  • HY-178061
    APS03118

    		ERK RET Cancer
    APS03118 is an orally active, potent and selective rearranged during transfection (RET) inhibitor. APS03118 broadly inhibits RET fusions and mutations (including G810, V804, L730, and Y806 variants), with IC50 values predominantly below 1 nM (0.095 nM for WT; ranging from 0.00438 to 5.72 nM for mutants), and demonstrates marked superiority against RET G810 mutations. APS03118 inhibits the entire RET signaling pathway (including RET, Shc, and ERK1/2), with >20-fold selectivity over most off-target kinases (except FLT3 and YES). APS03118 induces complete tumor regression in KIF5B-RET and CCDC6-RET V804 M patient derived xenografts (PDXs) and significantly prolongs survival in an intracranial CCDC6-RET metastasis mice model. APS03118 can be used for selective RET inhibitor (SRI)-resistant, RET-driven cancer research .
    APS03118
  • HY-170852
    QZ2135

    		PROTACs RET Cancer
    QZ2135 (compound 20) is a RET-targeted PROTAC degrader with in vivo antitumor properties in a Ba/F3-KIF5B-RET-G810C xenograft mouse model. The degradation activities of QZ2135 targeting KIF5B-RET have DC50 values of 4.7 nM (WT), 17.2 nM (V804M), and 73.8 nM (G810C), respectively. QZ2135 is composed of a target protein ligand (red part) RET ligand-3 (HY-170853), an E3 ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC Linker (black part) 7-Iodohept-1-yne (HY-W587352), in which the target protein ligand + linker form a conjugate RET Ligand-Linker Conjugate-1 (HY-170854) .
    QZ2135

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