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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 potent and allosteric inhibitor of oncogenic K-Ras(G12C). It binds to K-Ras(G12C) by forming a covalent bond with the 12C cysteine. Ras proteins belong to the large family of GTPase enzymes which are essential to transduce extracellular signals into diverse cellular responses including proliferation, differentiation, and apoptosis. About 30% of all human cancers contain activating Ras mutations, making them one of the most common known genetic molecular drivers of cancer. Therefore, K-Ras signaling have potential therapeutic advantages in cancer. 

    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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