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MK-1084

Chemical Structure : MK-1084

CAS No.: 2641216-67-1

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MK-1084 (Calderasib, MK1084)

Catalog No.: PC-22632Not For Human Use, Lab Use Only.

Calderasib (MK-1084) is a potent, orally bioavailable and low-dose KRAS G12C covalent inhibitor with IC50 of 1.2 nM in in vitro guanine nucleotide exchange assay, and 9 nM in cell-based phospho-ERK1/2 assay with H358 cell line.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    Calderasib (MK-1084) is a potent, orally bioavailable and low-dose KRAS G12C covalent inhibitor with IC50 of 1.2 nM in in vitro guanine nucleotide exchange assay, and 9 nM in cell-based phospho-ERK1/2 assay with H358 cell line.
    MK-1084 30 mg/kg QD dosing demonstrated excellent efficacy in patient-derived xenograft models, LU2512 and LU2529.

    Physicochemical Properties

    M.Wt 637.08
    Formula C32H31ClF2N6O4
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    1,18-Etheno-4H-pyrido[4,3-e]pyrimido[1,6-g][1,4,7,9]benzodioxadiazacyclododecin-4-one, 20-chloro-2-[(2S,5R)-2,5-dimethyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl]-14,17-difluoro-11,12-dihydro-6-(1-methylethyl)-, (5S,17aR)-

    References

    1. Ma X, et al. J Med Chem. 2024 Jun 26. doi: 10.1021/acs.jmedchem.4c00572.

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