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Results for "

MRTX849

" in MedChemExpress (MCE) Product Catalog:

7

Inhibitors & Agonists

1

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-130149
    Adagrasib
    15+ Cited Publications

    MRTX849

    		 Ras Cancer
    Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction .
    Adagrasib
  • HY-139402
    MRTX849 acid

    		Ras Cancer
    MRTX849 acid, a derivative of MRTX849, can be used in the synthesis of PROTAC LC-2 (HY-137516). LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC50s between 0.25 and 0.76 μM) .
    <em>MRTX849</em> acid
  • HY-139403
    MRTX849 ethoxypropanoic acid

    		Target Protein Ligand-Linker Conjugates Ras Cancer
    MRTX849 ethoxypropanoic acid incorporates a ligand for KRAS G12C, and a PROTAC linker. MRTX849 ethoxypropanoic acid can be used in the synthesis of PROTAC LC-2 (HY-137516). LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (IC50s between 0.25 and 0.76 μM) .
    <em>MRTX849</em> ethoxypropanoic acid
  • HY-137516A
    LC-2 epimer

    		PROTACs Ras Cancer
    LC-2 epimer is a differential isomer of LC-2. LC-2 is a mutation-selective PROTAC depressant for KRAS and contains a ligand for the von Hippel Lindau E3 ligase linked to the KRAS inhibitor MRTX849 .
    LC-2 epimer
  • HY-144323
    YF135

    		PROTACs PERK Cancer
    YF135 is an efficient and reversible-covalent KRAS G12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRAS G12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway .
    YF135
  • HY-137516
    LC-2
    1 Publications Verification

    		 PROTACs Ras Cancer
    LC-2 is a potent and first-in-class von Hippel-Lindau-based PROTAC capable of degrading endogenous KRAS G12C, with DC50s between 0.25 and 0.76 μM . LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines .
    LC-2
  • HY-145926
    MRTX0902

    		Ras Cancer
    MRTX0902 is an orally active and potent SOS1 inhibitor with an IC50 of 46 nM (WO2021127429A1; Example 12-10) .
    <em>MRTX</em>0902

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