Name: K-Ras(G12C) inhibitor 9
Price: 438.00 USD

- Overview
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    Background
    
    Target: K-Ras(G12C)IC50: N/AK-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C) [1]. 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 [2]. Therefore, K-Ras signaling have potential therapeutic advantages in cancer. K-Ras(G12C) is present in roughly 10–20% of Ras-driven cancers and in an estimated 50% of Ras-mutated lung adenocarcinomas [3].In vitro: 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) [1].In vivo: N/A
    
    1. Ostrem JM, Peters U, Sos ML, Wells JA, Shokat KM. K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions. Nature. 2013;503(7477):548-51.
    2. Hunter JC, Gurbani D, Ficarro SB, Carrasco MA, Lim SM, Choi HG, et al. In situ selectivity profiling and crystal structure of SML-8-73-1, an active site inhibitor of oncogenic K-Ras G12C. Proc Natl Acad Sci U S A. 2014;111(24):8895-900.
    3. Lim SM, Westover KD, Ficarro SB, Harrison RA, Choi HG, Pacold ME, et al. Therapeutic targeting of oncogenic K-Ras by a covalent catalytic site inhibitor. Angew Chem Int Ed Engl. 2014;53(1):199-204.
- Properties
  - Alternative Name
    
    N-(1-(2-((4-chloro-5-iodo-2-methoxyphenyl)amino)acetyl)piperidin-4-yl)ethenesulfonamide
    
    CAS Number
    
    1469337-91-4
    
    Molecular Formula
    
    C16H21ClIN3O4S
    
    Molecular Weight
    
    513.78
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    Soluble in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

K-Ras(G12C) inhibitor 9

K-Ras(G12C) inhibitor 9

Background

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