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

CAS: 10161-87-2 Cat. No.: K654869 分子式: C₁₃H₁₆BrNO₃ 分子量: 314.18 PubChem CID: 270269

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

概要

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

仕様と純度

10mM in DMSO

生化学的・生理学的メカニズム

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

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

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アクションタイプ

AGONIST

名前と識別子

• 異性体SMILES: C1=CC(=CC=C1CCCCNC(=O)CBr)C(=O)O
• 代替CAS番号: 10161-87-2
• PubChem CID: 270269
• NSC番号: 112533
• 分子量: 314.18

よくある質問

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 10161-87-2, the molecular formula is C13H16BrNO3, and the molecular weight is 314.18 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.