p53-MDM2-IN-5
p53-MDM2-IN-5 (compound 5a) is a potent p53-MDM2 inhibitor. p53-MDM2-IN-5 induces apoptosis, autophagy and DNA damage. p53-MDM2-IN-5 induces cell cycle arrest at S and G2/M phases. p53-MDM2-IN-5 shows anti-tumor activity.
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- CAS. Nr.: 2750075-06-8
- Formel: C33H37Cl4F2N5O6Pt
- Molecular Weight:974.57
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
In Vitro
p53-MDM2-IN-5 (compound 5a) (1-5 µM; 24 h) induces apoptosis and cell cycle arrest at S and G2/M phases in A549 cells[1].
p53-MDM2-IN-5 (1, 5 µM; 24 h) induces autophagy by decreases the expression of SQSTM1/p62[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549, A549/CDDP, Panc-1, CFPAC-1, SJSA-1, HepG2, HCT116, HLF-1 cells
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Concentration:0-100 µM
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Incubation Time:24 h
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Result:Inhibited cell growth with IC50s of 0.85, 1.43, 2.22, 1.64, 0.14, 6.23, 2.57, 18.94 µM for A549, A549/CDDP, Panc-1, CFPAC-1, SJSA-1, HepG2, HCT116, HLF-1 cells, respectively.
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Cell Line:A549 cells
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Concentration:1 µM
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Incubation Time:24 h
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Result:Induced cell cycle arrest at S and G2/M phases.
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Cell Line:A549 cells
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Concentration:0.1, 0.5, 1 µM
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Incubation Time:24 h
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Result:Induced apoptosis with the percentages of apoptotic cells of 8.1%, 11.4%, and 15.1% at 0.1, 0.5, 1 µM, respectively.
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Cell Line:A549 cells
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Concentration:1, 5 µM
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Incubation Time:24 h
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Result:Induced autophagy by promoted the conversion of LC3B-I to LC3B-II and decreased the expression of SQSTM1/p62.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6–8-week-old female nude mouse (A549 xenograft nude mouse model)[1]
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Dosage:6 μmol/kg
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Administration:I.v.; every 3 days for 21 days
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Result:Inhibited tumor growth with low toxicity.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Autophagy
- Apoptosis Solutions
- Protocol for Cell Cycle
- Lysosome and acidic-vesicle live-cell staining
- Macroautophagy Solutions
- Genotoxicity/Mutagenicity Study
Chemical Information
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CAS. Nr. 2750075-06-8
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Molecular Weight 974.57
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Formel C33H37Cl4F2N5O6Pt
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SMILES
N#C[C@@]1(C2=C(C=C(C=C2)Cl)F)[C@@H](C3=C(C(Cl)=CC=C3)F)[C@@H](N[C@H]1CC(C)(C)C)C(NC4=C(C=C(C=C4)C([O-][Pt+4]([Cl-])([Cl-])([NH3])([NH3])[O-]C(C)=O)=O)OC)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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