MS9427 is a potent PROTAC EGFR degrader with K d s of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer
In Vitro
MS9427 has antiproliferative activity against HCC-827 cells, with a GI 50 of 0.87 ± 0.27 μM. MS9427 (0-10 μM, 16 h) potently induces EGFR Del19 degradation (DC 50 =82 ± 73 nM) and inhibits EGFR phosphorylation (p-EGFR) in a concentration-dependent manner in HCC-827 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: HCC-827 cells Concentration: 1, 10, 50, 100, 200, 500, 100, and 10000 nM Incubation Time: 16 h Result: Inhibited EGFR phosphorylation (p-EGFR) in a concentration-dependent manner in HCC-827 cells. Western Blot AnalysisCell Line: HCC-827 cells Concentration: 100 nM Incubation Time: 1, 2, 4, 6, 12, 24, 48 h Result: Induced EGFR degradation in a time-dependent manner and through the UPS and autophagy/lysosome system.
MS9427 is a potent PROTAC EGFR degrader with K d s of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways
Condições de armazenamento de armazenamento
Store at 2-8°C,Protected from light,Argon charged
Enviado em
Wet ice
Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.
Tipo de ação
DEGRADER
Pureza
≥95%
Nomes e identificadores
Peso molecular
993.47
Dados avançados
Certificados(CoA,COO,BSE/TSE e Mapa de Análise)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
Propriedades químicas e físicas
Solubilidade
DMSO : 70 mg/mL (70.46 mM; Need ultrasonic)
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Revisões
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Perguntas frequentes
What is the purity of this product?
This product is supplied at ≥95% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.
How should this product be stored?
Store at 2–8 °C, protected from light, under argon. It is supplied under an argon blanket; reseal under inert gas after each use.
How is this product shipped?
This product ships chilled on wet ice. Unpack on arrival and transfer it to the storage condition stated above.
What are the CAS number, molecular formula and molecular weight?
The CAS Number is 2772613-37-1, the molecular formula is C48H58ClFN8O12, and the molecular weight is 993.47 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.
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