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G12Si-5

Chemical Structure : G12Si-5

CAS No.: 2946593-46-8

G12Si-5 (K-Ras(G12S) inhibitor)

Catalog No.: PC-49153Not For Human Use, Lab Use Only.

G12Si-5 is a specific small molecule that covalently targets K-Ras(G12S) mutation, suppresses K-Ras(G12S) signaling, preferentially inhibits the growth of the K-Ras(G12S)-transduced cells with IC50 of 2.4 uM.

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

    Biological Activity

    G12Si-5 is a specific small molecule that covalently targets K-Ras(G12S) mutation, suppresses K-Ras(G12S) signaling, preferentially inhibits the growth of the K-Ras(G12S)-transduced cells with IC50 of 2.4 uM.
    G12Si-5 inhibits Ras signaling in A549 cells with IC50 of 3 uM, does not perturb the signaling in A375 cells (wild-type KRAS) or SW1990 cells (homozygous KRAS p.G12D).
    G12Si-5 dose-dependently reduces phospho-ERK levels in Ba/F3:K-Ras(G12S) cells, also inhibits the growth of KMS20, a patient-derived myeloma cell line with a homozygous KRAS p.G12S mutation, with IC50 of 7.5 uM.

    Physicochemical Properties

    M.Wt 574.053
    Formula C31H29ClFN5O3
    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

    (1R,6R)-3-(7-(8-chloronaphthalen-1-yl)-8-fluoro-2-((tetrahydro-1H-pyrrolizin-7a(5H)-yl)methoxy)pyrido[4,3-d]pyrimidin-4-yl)-8-oxa-3-azabicyclo[4.2.0]octan-7-one

    References

    1. Ziyang Zhang, et al. Nat Chem Biol. 2022 Jul 21. doi: 10.1038/s41589-022-01065-9.

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