KRA-533

CAS No. 10161-87-2

KRA-533( ——— )

Catalog No. M39441 CAS No. 10161-87-2

KRA-533 is a potent KRAS agonist. KRA-533 binds to the GTP/GDP binding pocket in the KRAS protein to prevent GTP cleavage, resulting in the accumulation of constitutively active GTP-bound KRAS that triggers both apoptotic and autophagic cell death pathways in cancer cells.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    KRA-533
  • Note
    Research use only, not for human use.
  • Brief Description
    KRA-533 is a potent KRAS agonist. KRA-533 binds to the GTP/GDP binding pocket in the KRAS protein to prevent GTP cleavage, resulting in the accumulation of constitutively active GTP-bound KRAS that triggers both apoptotic and autophagic cell death pathways in cancer cells.
  • Description
    KRA-533 is a potent KRAS agonist. KRA-533 binds to the GTP/GDP binding pocket in the KRAS protein to prevent GTP cleavage, resulting in the accumulation of constitutively active GTP-bound KRAS that triggers both apoptotic and autophagic cell death pathways in cancer cells.
  • In Vitro
    Western Blot Analysis Cell Line:HCC827 cells Concentration:10 μM Incubation Time:48 hours Result:Enhanced KRAS activity to a greater extent. Apoptosis Analysis Cell Line:H157 cells Concentration: 0~15 μM Incubation Time:48 hours Result:Enhanced KRAS activity in a dose-dependent manner, which was associated increased levels of pERK, ratio of active caspase 3/procaspase 3 and PARP cleavage, leading to apoptotic cell death.
  • In Vivo
    Animal Model:Nu/Nu nude mice (mutant KRAS xenografts) Dosage:0~30 mg/kg Administration:i.p.; 28 days Result:Suppressed tumor growth in a dose-dependent manner in lung cancer mutant KRAS xenografts and induced apoptosis and autophagy in tumor tissues in a dose-dependent manner.
  • Synonyms
    ———
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    KRAS
  • Research Area
    ———
  • Indication
    ———

Chemical Information

  • CAS Number
    10161-87-2
  • Formula Weight
    314.179
  • Molecular Formula
    C13H16BrNO3
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : 250 mg/mL (795.72 mM; ultraphonic; )
  • SMILES
    ———
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Xu K, et al. Small Molecule KRAS Agonist for Mutant KRAS Cancer Therapy published correction appears in Mol Cancer. 2020 May 20;19(1):93. Mol Cancer. 2019;18(1):85. Published 2019 Apr 10.?
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