Name: K-Ras(G12C) inhibitor 12
Price: 280.00 USD

- Overview
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    Background
    
    K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of K-Ras(G12C) [1].
    K-Ras is a GTPase and plays an important role in many signal transduction pathways. The mutation of K-Ras occurs in many cancers.
    K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of K-Ras(G12C). K-Ras(G12C) exhibited a slight preference for GTP. However, K-Ras(G12C) inhibitor 12 significantly reduced the affinity for GTP and led to the modification of K-Ras(G12C). Also, K-Ras(G12C) inhibitor 12 inhibited SOS-catalysed nucleotide exchange. In H1792 and H358 K-Ras(G12C)-mutant lung cancer cell lines, K-Ras(G12C) inhibitor 12 reduced the association of C-Raf and B-Raf with Ras. In H1792, H358, H23 and Calu-1 cell lines containing G12C mutations, K-Ras(G12C) inhibitor 12 decreased viability and induced apoptosis. K-Ras(G12C) inhibitor 12 exhibited EC50 value of 0.32 µM in H1792 cells. Also, the H1792 cells exhibited low levels of K-Ras GTP, which was consistent with the preference of K-Ras(G12C) inhibitor 12 to K-Ras GDP [1].
- Properties
  - Alternative Name
    
    1-[4-[2-(4-chloro-2-hydroxy-5-iodoanilino)acetyl]piperazin-1-yl]prop-2-en-1-one
    
    CAS Number
    
    1469337-95-8
    
    Molecular Formula
    
    C15H17ClIN3O3
    
    Molecular Weight
    
    449.67
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥8.98 mg/mL in DMSO with gentle warming
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Chen Z, Yang D, et al. "Final-2 targeted glycolysis mediated apoptosis and autophagy in human lung adenocarcinoma cells but failed to inhibit xenograft in nude mice." Food Chem Toxicol. 2019 Aug;130:1-11. PMID:31054290

K-Ras(G12C) inhibitor 12

K-Ras(G12C) inhibitor 12

Background

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