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    K-Ras(G12C) inhibitor 9
    K-Ras(G12C) inhibitor 9

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1572
    CAS #: 1469337-91-4Purity ≥98%

    Description: K-Ras(G12C) inhibitor 9 is a novel, covalent and allosteric inhibitor of K-RAS G12C mutant with potential anticancer activity. It binds covalently to K-RAS G12C and forms a covalent bond with cysteine residue at position 12. Ras mutations are found in about 30% of all human cancers and have become an excellent target for anticancer therapeutics. 

    References: Nature. 2013 Nov 28;503(7477):548-51.

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    Molecular Weight (MW)513.78
    FormulaC16H21ClIN3O4S 
    CAS No.1469337-91-4
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 53 mg/mL (103.1 mM)
    Water: <1 mg/mL
    Ethanol:<1 mg/mL
    Other info

    Chemical Name: N-[1-[2-[(4-Chloro-5-iodo-2-methoxyphenyl)amino]acetyl]-4-piperidinyl]ethenesulfonamide

    InChi Key: ZGUSBCDCZNBNQT-UHFFFAOYSA-N

    InChi Code: InChI=1S/C16H21ClIN3O4S/c1-3-26(23,24)20-11-4-6-21(7-5-11)16(22)10-19-14-9-13(18)12(17)8-15(14)25-2/h3,8-9,11,19-20H,1,4-7,10H2,2H3

    SMILES Code: C=CS(=O)(NC1CCN(C(CNC2=CC(I)=C(Cl)C=C2OC)=O)CC1)=O           

    SynonymsK-Ras(G12C) inhibitor 9 


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    In Vitro

    In vitro activity: K-Ras(G12C) inhibitor 9 belongs to a series of small molecules, which irreversibly bind to a common oncogenic mutant K-Ras(G12C) and blocks K-Ras(G12C) interactions. Some of them decrease viability and increase apoptosis of G12C-containing cancer cell lines


    Cell Assay:  K-Ras(G12C) inhibitor 9 belongs to a series of small molecules, which irreversibly compete with GTP and GDP for binding to a common oncogenic K-Ras(G12C) mutant and blocked the association of B-Raf and C-Raf with K-Ras(G12C). K-Ras(G12C) inhibitor 9 (10 μM) decreased viability and increased apoptosis of G12C mutations-containing lung cancer cell lines (H1792, Calu-1, H358, and H23)

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    References

    Nature. 2013 Nov 28;503(7477):548-51.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    K-Ras(G12C) inhibitor 12

    Inhibitor sensitivity, K-Ras GTP levels and K-Ras dependency of lung cancer cell lines.Nature. 2013 Nov 28;503(7477):548-51.
     

    K-Ras(G12C) inhibitor 12

    Tethering compounds selectively bind to oncogenic K-Ras(G12C). Nature. 2013 Nov 28;503(7477):548-51.


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