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    K-Ras inhibitor 12
    K-Ras inhibitor 12

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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 #: V1570
    CAS #: 1469337-95-8Purity ≥98%

    Description: K-Ras(G12C) inhibitor 12 is a co-valent and allosteric inhibitor of K-Ras G12C with potential antitumor activity. KRAS G12C is the mutated form of K-ras and is oncogenic. K-Ras(G12C) inhibitor 12 acts by binding to K-Ras(G12C) and forming a covalent bond with the 12C cysteine of KRAS. 

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

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    Molecular Weight (MW)449.67
    FormulaC15H17ClIN3O3
    CAS No.1469337-95-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 27 mg/mL (60.0 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: 1-(4-(2-((4-Chloro-2-hydroxy-5-iodophenyl)amino)acetyl)piperazin-1-yl)prop-2-en-1-one

    InChi Key: JFIFBWVNHLXJFY-UHFFFAOYSA-N

    InChi Code: InChI=1S/C15H17ClIN3O3/c1-2-14(22)19-3-5-20(6-4-19)15(23)9-18-12-8-11(17)10(16)7-13(12)21/h2,7-8,18,21H,1,3-6,9H2

    SMILES Code: C=CC(N1CCN(C(CNC2=CC(I)=C(Cl)C=C2O)=O)CC1)=O           

    SynonymsK-Ras(G12C) inhibitor 12; K-Ras(G12C) inhibitor


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    In Vitro

    In vitro activity: K-Ras(G12C) inhibitor 12 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 12 is a highly effective Ras inhibitor and its EC50 value in H1792 cells is 0.32 μM.It selectively binds to an oncogenic mutant K-Ras(G12C) in a irreversible manner without affecting the activity of wild-type Ras. After treatment with K-Ras(G12C) inhibitor 12, K-Ras(G12C)-mutant cells exhibit decreased viability and increased apoptosis comparing to cells lacking this mutation.

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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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