K-Ras(G12C) inhibitor 6

K-Ras(G12C) inhibitor 6

Catalog Number:
L002370576APE
Mfr. No.:
APE-B3694
Price:
$277
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      • Overview
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          Background

          K-Ras (G12C) inhibitor 6 is an allosterical inhibitor of oncogenic mutation K-Ras G12C [1].K-Ras (G12C) inhibitor 6 is a cysteine-reactive small molecule. It irreversibly binds to the G12C mutantion of GTPase K-Ras but not the wild-type K-Ras with the relative potency value of 4.2. The binding pocket of K-Ras for K-Ras (G12C) inhibitor 6 is a new allosteric pocket, S-IIP. Binding of this pocket results in a change of the relative nucleotide affinity of Ras to favour GDP over GTP, leading to an accumulation of inactive Ras. Since the mutation of K-Ras is quite common in human cancers, the inhibitor of K-Ras G12C should exert suppression activities in tumor cells. It has been reported that, some of the K-Ras G12C inhibitors are indeed effective to decrease cell viability and increase apoptosis in lung cancer cell lines [1].

          [1] Ostrem J M, Peters U, Sos M L, et al. K-Ras (G12C) inhibitors allosterically control GTP affinity and effector interactions. Nature, 2013, 503(7477): 548-551.

      • Properties
        • CAS Number
          2060530-16-5
          Molecular Formula
          C17H22Cl2N2O3S
          Molecular Weight
          405.34
          Appearance
          A solid
          Purity
          98.10%
          Solubility
          insoluble in H2O; insoluble in EtOH; ≥20.25 mg/mL in DMSO
          Storage
          Store at -20°C

          * For Research Use Only

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