Antitumor agent-217
Antitumor agent-217 is a dual mitochondria-targeted anticancer agent. Antitumor agent-217 exhibits potent and selective antiproliferative activity against bladder cancer cell line J82 (IC50 = 6.3 μM), and inhibits colony formation and migration of J82 cells. Antitumor agent-217 accumulates in mitochondria, alters mitochondrial morphology, reduces ATP production, increases ROS generation and decreases mitochondrial membrane potential. Antitumor agent-217 induces apoptosis (Apoptosis) and ferroptosis (Ferroptosis) in bladder cancer cells. Antitumor agent-217 can be used for the research of bladder cancer.
For research use only. We do not sell to patients.
- Formula: C32H36BrClN5O2P
- Molecular Weight:668.99
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Bcl-2 |
Antitumor agent-217 (compound 7f) (Range of concentrations; 72 h) inhibits viability of OVCAR3, SKOV3, J82, T24, and A549 cancer cells with highest potency against J82 cells (IC50 = 6.3 μM) and high selectivity over normal SV-HUC-1 cells[1].
Antitumor agent-217 (1.5-6 μM; 6-8 days) dose-dependently inhibits colony formation of J82 bladder cancer cells[1].
Antitumor agent-217 (1.5-6 μM; 24-48 h) dose-dependently inhibits migration of J82 bladder cancer cells[1].
Antitumor agent-217 (10 μM; 4 h) accumulates in mitochondria of J82 bladder cancer cells[1].
Antitumor agent-217 (8 μM; 48 h) disrupts mitochondrial morphology in J82 bladder cancer cells, causing swelling, membrane rupture, and cristae loss[1].
Antitumor agent-217 (2-8 μM; 48 h) reduces ATP production and mitochondrial membrane potential, increases intracellular ROS levels, upregulates pro-apoptotic protein BAX and downregulates anti-apoptotic protein BCL-2, and suppresses NRF2/SLC7A11/GPX4 signaling along with elevated lipid peroxidation and MDA levels and decreased GSH levels, thereby inducing apoptosis and ferroptosis in J82 bladder cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:J82 human bladder cancer cells
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Concentration:1.5, 3, 6 μM
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Incubation Time:6-8 days
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Result:Dose-dependently inhibited colony formation of J82 cells, with significant inhibition at all tested concentrations compared to untreated controls.
Showed slightly greater inhibitory potency than cisplatin at equal concentrations.
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Cell Line:J82 human bladder cancer cells
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Concentration:1.5, 3, 6 μM
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Incubation Time:24 h, 48 h
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Result:Significantly reduced the migration ability of J82 cells, with dose-dependent inhibition of wound closure at 24 and 48 h compared to untreated controls.
Exhibited an inhibitory effect comparable to that of cisplatin.
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Cell Line:J82 human bladder cancer cells
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Concentration:2, 4, 8 μM
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Incubation Time:48 h
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Result:Induced 5.02% early apoptosis and 47.5% late apoptosis in J82 cells at 8 μM, with total apoptosis reaching ~52.5%.
Dose-dependently upregulated pro-apoptotic BAX protein and downregulated anti-apoptotic BCL-2 protein, with the BAX/GAPDH ratio increasing to ~1.7 and the BCL-2/GAPDH ratio decreasing to ~0.5 at 8 μM compared to control.
Chemical Information
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Molecular Weight 668.99
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Formula C32H36BrClN5O2P
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SMILES
O=C(OCCC1=CC=CC(/N=C(N)/N=C(N)/N)=C1)CCC[P+](C2=CC=CC=C2)(C3=CC=CC=C3)C4=CC=CC=C4.[Br-].Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Antitumor agent-217 Related Classifications
HY-183312 Related Classifications
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