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KRA-533

SKU: orb3054179

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.

Images & Validation

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KRA-533

Key Properties

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CAS Number10161-87-2
MW314.179
Purity>98% (HPLC)
FormulaC13H16BrNO3
SolubilityDMSO : 250 mg/mL (795.72 mM; ultraphonic; )

Bioactivity

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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.
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.

Storage & Handling

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StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

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  • KRA-533 [orb1692029]

    10161-87-2

    314.179

    C13H16BrNO3

    2 mg
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2 mg
$ 240.00
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