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Adagrasib

(Synonyms: MRTX849)
63 Cited Publications
고객리뷰

Based on 63 publication(s) in Google Scholar

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.

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  • Purity: 99.96%
  • CAS No.: 2326521-71-3
  • 화학식: C32H35ClFN7O2
  • 분자량:604.12
  • 보관:
    Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -80°C, 6 months , -20°C, 1 month
  • Adagrasib Chemical Structure
    Adagrasib Chemical Structure
  • Experimental Validation Results for Adagrasib
  • Experimental Validation Results for Adagrasib
  • Experimental Validation Results for Adagrasib
  • Experimental Validation Results for Adagrasib
CAS No.: 2326521-71-3
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  • Adagrasib Chemical Structure
    Adagrasib Chemical Structure
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  • 1/16

    Adagrasib purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2024 May 8. [Abstract]

    Customer Validation
     Adagrasib (78 nM; 2 h). Cellular activity of KRAS G12C inhibitors in NCI-H358 NSCLC cells was evaluated through active RAS-GTP pull-down followed by immunoblotting using a KRAS-specific antibody after a 2-hour treatment with different inhibitors at indicated concentrations. The levels of active KRAS were quantified by chemiluminescence intensity, and IC50 values were calculated using GraphPad Prism for each compound.

  • 1/16

    Adagrasib purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2024 Sep;5(9):1352-1370. [Abstract]

    Customer Validation
     Adagrasib (150 nM, 6-24 h) inhibits KRAS-GTP activity in NCI-H2122 and NCI-H358 cells, but compensatory activation of WT RAS isoforms (including NRAS and MRAS) is observed following monotherapy.

  • 1/16

    Adagrasib purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2023 Jun;4(6):829-843. [Abstract]

    Customer Validation
     The NCI-H358 KRAS G12C mutant lung cancer cell line was treated with 500 nM Adagrasib for 48 hours. Representative immunofluorescence images of E-cadherin are shown. Scale bar, 10 μm.

  • 1/16

    Adagrasib purchased from MedChemExpress. Usage Cited in: bioRxiv. 2023 Feb 18:2023.02.15.528757. [Abstract]

    Customer Validation
     Adagrasib (MRTX849; 60 nM-1 µM) induces Fas expression in KrasG12C mutant MIA PaCa-2 cells.

  • Adagrasib