Antitumor agent-77
Antitumor agent-77 is an antitumor agent, inhibits cancer cells growth and migration. Antitumor agent-77 triggers ferroptosis by inhibiting GPx-4 and elevating COX2. Antitumor agent-77 also activates intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and hinders Epithelial-mesenchymal transition (EMT) process of cancer cells.
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- No. CAS: 2870703-21-0
- Fòrmula: C7H11F3N2O5Pt
- Peso molecular:455.25
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Almacenamiento:
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Actividad biológica
Descripciòn
IC50 & Target
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COX-2 |
Bax |
Bcl-2 |
In Vitro
Antitumor agent-77 (compound 2a) (30 μM; 4 h) exhibits better solubility and improved cellular uptake than Carboplatin (HY-17393) in A549 cells[1].
Antitumor agent-77 (20 μM; 36 h) produces cytotoxicity by inducing apoptosis of A549 cancer cells[1].
Antitumor agent-77 (20 μM; 24 h) results in significant down-regulation of Bcl-2 and upregulation of Bax, also leads to E-cadherin increase, Vimentin decrease[1].
Antitumor agent-77 (20 μM; 24 h) arrests cell cycle at S phase and G2/M phase[1].
Antitumor agent-77 (10 μM; 12 h) inhibits cells migration with inhibition rate of 52%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cells
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Concentration:20 μM
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Incubation Time:36 hours
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Result:Resulte cell apopsotsis with average apoptotic values (including both early and late apoptotic states which were displayed in Q1-LR and Q1-UR, respectively) of 25.34%.
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Cell Line:A549 cells
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Concentration:20 μM
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Incubation Time:24 hours
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Result:Elevated the level of cleaved caspase-3 and reduced the level of caspase-3 in A549 cells.
Decreased anti-apoptotic protein Bcl-2 and increased pro-apoptotic protein Bax.
Elevated the expression of E-cadherin and on the other hand, lowered the protein level of Vimentin.
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Cell Line:A549 cells
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Concentration:20 μM
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Incubation Time:24 hours
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Result:Blocked cell cycle progression in S and G2/M phase with the values of 41.11% and 26.03%, respectively.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A549 xenograft models in mouse[1]
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Dosage:6 μg/kg
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Administration:Intravenous injection; administration on day 8, 10, 12 after establishing xenograft models (A549 cells; s.c.)
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Result:Significantly repressed tumor growth, and maintained normal kidney and liver architecture in mice.
Chemical Information
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No. CAS 2870703-21-0
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Peso molecular 455.25
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Fòrmula C7H11F3N2O5Pt
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SMILES
O=C1[O-][Pt+2]([NH3])([NH3])[O-]C(C12CC(C2)(C(F)(F)F)O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
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Ficha de datos (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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Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Antitumor agent-77 Related Classifications
HY-151429 Related Classifications
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