Ferroptosis/apoptosis inducer-4
Ferroptosis/apoptosis inducer-4 is a pyridine-hydrazone-derived Cu (II) complex and a synergistic inducer of ferroptosis and apoptosis. Ferroptosis/apoptosis inducer-4 exerts anti-tumor proliferation and anti-metastasis effects with extremely low systemic toxicity. Ferroptosis/apoptosis inducer-4 disrupts cellular redox homeostasis by depleting glutathione and generating hydroxyl radicals through the Cu2+/Cu+ redox cycle. Ferroptosis/apoptosis inducer-4 also triggers mitochondrial dysfunction and endoplasmic reticulum stress, which in turn lead to Ca2+ release, mitochondrial Ca2+ overload, and the formation of a ROS−Ca2+ self-amplifying feedback loop. Ferroptosis/apoptosis inducer-4 can be used in studies related to cervical cancer.
For research use only. We do not sell to patients.
- Formula: C14H15Br2CuFN4
- Molecular Weight:481.65
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Ferroptosis/apoptosis inducer-4 (Cu2) (incubated for 24 h) potently inhibits the viability of HeLa, MCF-7, SK-OV-3, A549 and HCT-116 tumor cells, with IC50s ranging from 0.39 μM to 1.44 μM, and exhibits low cytotoxicity against normal LX-2 cells[1].
Ferroptosis/apoptosis inducer-4 (0.4-0.8 μM) induces caspase-dependent apoptosis in HeLa cells by altering the expression of pro-apoptotic and anti-apoptotic proteins, and activating caspase-3 and caspase-9 in a dose-dependent manner[1].
Ferroptosis/apoptosis inducer-4 (0.4-0.8 μM) inhibits the migration and invasion of HeLa cells in a dose-dependent manner, and this effect is associated with the downregulated expression of MACC1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | AUC0-24 | T1/2 | Tmax | Cmax |
|---|---|---|---|---|---|---|
| Mice[1] | 5 mg/kg | i.v. | 25.6 mg·h/L | 38.9 h | 0.5 h | 25.7 mg/L |
Cu2+ (5 mg/kg; i.v.) effectively inhibits HeLa cell lung metastasis in nude mice, as evidenced by reduced lung metastatic burden and lower lung wet weight[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice with Cervical cancer[1]
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Dosage:5 mg/kg
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Administration:i.v.; every other day
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Result:Achieved a tumor growth inhibition rate (TGI) of 64.7%.
Showed continued body weight increase during treatment.
Showed no statistically significant differences in major organ (heart, liver, spleen, lung, kidney) weights compared to control mice.
Showed no obvious pathological damage observed in H&E-stained organ sections.
Chemical Information
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Molecular Weight 481.65
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Formula C14H15Br2CuFN4
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SMILES
CC(C1=[N]2NC3=[N]([Cu+2]2([Br-])([N]4=C1C=CC=C4)[Br-])C=CC(F)=C3)C
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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)