Platinum(IV) Prodrug-1
Platinum (IV) Prodrug-1 is a Pt (IV) prodrug and selective TrxR1 inhibitor. Platinum (IV) Prodrug-1 induces ferroptosis (Ferroptosis) by depleting glutathione, accumulating intracellular lipid peroxides, and inactivating Glutathione peroxidase 4. Platinum (IV) Prodrug-1 triggers endoplasmic reticulum stress and immunogenic cell death via excessive accumulation of intracellular ROS. Platinum (IV) Prodrug-1 exhibits anticancer activity against both Cisplatin (HY-17394)-sensitive and Cisplatin-resistant triple-negative breast cancer cells. Platinum (IV) Prodrug-1 can be used for the research of triple-negative breast cancer.
For research use only. We do not sell to patients.
- Formula: C26H26Cl3F6N3O4Pt
- Molecular Weight:859.94
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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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TrxR1 |
GPX4 |
Platinum(IV) Prodrug-1 (Compound 6b) (2.5-5 μM; 24 h) induces concentration-dependent mitochondrial membrane potential reduction and activates the mitochondrial apoptosis pathway in Cisplatin-resistant MDA-MB-231/CDDP cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Platinum (IV) Prodrug-1 (7.2 mg/kg; intravenous injection; once every 2 days; for 21 consecutive days) exhibits potent in vivo anti-tumor activity in cisplatin-sensitive MDA-MB-231 triple-negative breast cancer (TNBC) xenograft-bearing BALB/c nude mice, with a tumor growth inhibition (TGI) rate of 73.8%, and no organ toxicity is observed[1].
Platinum (IV) Prodrug-1 (7.2 mg/kg; intravenous injection; once every 2 days; for 21 consecutive days) exhibits potent in vivo antitumor activity in cisplatin-resistant MDA-MB-231/CDDP triple-negative breast cancer (TNBC) xenograft-bearing BALB/c nude mice, with a tumor growth inhibition (TGI) rate of 66.3%, and no organ toxicity is observed[1].
Platinum (IV) Prodrug-1 (7.2 mg/kg; intravenous injection; once every 2 days; for 14 consecutive days) effectively inhibits lung metastasis of 4T1 triple-negative breast cancer (TNBC) cells in BALB/c mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 4 weeks old, ~20 g, subcutaneous inoculation of 4T1 murine breast cancer cells)[1]
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Dosage:7.2 mg/kg
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Administration:i.v.; once every 2 days; 21 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 76.8%.
Showed no significant body weight loss in treated mice.
Increased proportions of tumor-infiltrating lymphocytes: CD3+ T cells (23.46%), CD3+CD4+ T cells (14.40%), and CD3+CD8+ T cells (8.85%).
Increased CD80+CD86+ dendritic cells (56.78%) relative to control.
Elevated serum levels of proinflammatory cytokines TNF-α, IFN-γ, and IL-6 significantly compared to other treatment groups.
Increased levels of the ICD marker CRT and ER stress marker CHOP in tumor tissue via immunofluorescence staining.
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Animal Model:BALB/c nude (female, 4−5 weeks old, ~18 g, subcutaneous inoculation of MDA-MB-231 human breast cancer cells)[1]
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Dosage:7.2 mg/kg
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Administration:i.v.; once every 2 days; 21 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 73.8%.
Showed no significant body weight loss in treated mice.
Downregulated Ki67, TrxR1, and GPX4 expression significantly in tumor tissue relative to control and other treatment groups.
Showed no morphological alterations or adverse effects in major organs (heart, liver, spleen, lung, kidney) via H&E staining.
Chemical Information
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Molecular Weight 859.94
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Formula C26H26Cl3F6N3O4Pt
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SMILES
O=C(CCCC(O[Pt]([NH3])(Cl)(Cl)([NH3])Cl)=O)N1C/C(C(/C(C1)=C/C2=CC(C(F)(F)F)=CC=C2)=O)=C\C3=CC=CC(C(F)(F)F)=C3
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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)
Platinum(IV) Prodrug-1 Related Classifications
HY-183544 Related Classifications
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