KRA-533 - 10mM in DMSO , CAS No.10161-87-2

CAS: 10161-87-2 Cat. No.: K654869 Peso molecular: 314.18 PubChem CID: 270269

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

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

KRA-533 (10 μM; 48 hours; HCC827 cells) enhances KRAS activity to a greater extent. KRA-533 (0~15 μM; 48 hours; H157 cells) enhances KRAS activity in a dose-dependent manner, which is associated increased levels of pERK, ratio of active caspase 3/procaspase 3 and PARP cleavage, leading to apoptotic cell death. KRA-533 (10 μM; 10 days; H292 cells) mediates cell growth suppression than those without KRAS mutation. KRA-533 (5~15 μM) can directly bind to WT, G12C, G12D and G13D mutant KRAS proteins. KRA-533 activates WT KRAS to increase its activity in a dose-dependent manner. KRA-533 further enhances the activities of active KRAS mutants. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: HCC827 cells Concentration: 10 μM Incubation Time: 48 hours Result: Enhanced KRAS activity to a greater extent. Apoptosis AnalysisCell 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

KRA-533 (0~30 mg/kg; i.p.; 28 days) suppresses tumor growth in a dose-dependent manner in lung cancer mutant KRAS xenografts and induces apoptosis and autophagy in tumor tissues in a dose-dependent manner . KRA-533 shows optimal therapeutic index between 7.5 mg/kg and 30 mg/kg doses . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.

IC50& Target:KRAS

Specifications

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

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 pathway

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Tipo de acción

AGONIST

Nombres e identificadores

• Isómeros SMILES: C1=CC(=CC=C1CCCCNC(=O)CBr)C(=O)O
• CAS alternativo: 10161-87-2
• PubChem CID: 270269
• Número NSC: 112533
• Peso molecular: 314.18