Theophylline-platinum(IV) prodrug-1
Theophylline-platinum(IV) prodrug-1 is a PARP-1 inhibitor. Theophylline-platinum(IV) prodrug-1 enhances DNA damage, ROS production, mitochondrial dysfunction, apoptosis and S-phase arrest, along with reducing invasion and metastasis in cells. Theophylline-platinum(IV) prodrug-1 exhibits superior antitumor activity in the xenograft SKOV3-BRCA1-KD tumor model. Theophylline-platinum(IV) prodrug-1 can be used for the study of ovarian cancer.
For research use only. We do not sell to patients.
- Formula: C25H46Cl2N6O6Pt
- Molecular Weight:792.66
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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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Biological Activity
Description
In Vitro
Theophylline-platinum(IV) prodrug-1 (Compound 4) (10-7-1 nM, 72 h) inhibits the proliferation of SKOV3 cells (IC50 = 0.13 μM), SKOV3-BRCA1-KD cells (IC50 = 0.1 μM), A549 cells (IC50 = 0.31 μM), A549-BRCA1-KD cells (IC50 = 0.18 μM), MCF-7 cells (IC50 = 0.10 μM), MCF-7-BRCA1-KD cells (IC50 = 0.04 μM), MDA-MB-231 cells (IC50 = 0.08 μM), IOSE-80 cells (IC50 = 0.18 μM) and SI cells (IC50 = 18 μM)[1].
Theophylline-platinum(IV) prodrug-1 (10 μM, 6 h) induces DNA damage in SKOV3 and SKOV3-BRCA1-KD cells[1].
Theophylline-platinum(IV) prodrug-1 (0.5-2 μM, 24 h) induces ROS production, mitochondrial membrane potential damage, cell cycle arrest and apoptosis in SKOV3 and SKOV3-BRCA1-KD cells[1].
Theophylline-platinum(IV) prodrug-1 (0.5 μM, 24 h) induces invasion and metastasis inhibition in SKOV3 and SKOV3-BRCA1-KD cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SKOV3 and SKOV3-BRCA1-KD cells
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Concentration:0.5, 1, 10 μM
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Incubation Time:6, 24 h
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Result:Induced a remarkable 15.13-fold increase in γH2AX foci formation in SKOV3-BRCA1-KD cells.
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Cell Line:SKOV3 and SKOV3-BRCA1-KD cells
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Concentration:1 μM
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Incubation Time:24 h
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Result:Resulted in an S-phase cell proportion of 38.67% in SKOV3 cells and led to an S-phase cell proportion of 63.52% in BRCA1-deficient cells.
Showed S-phase arrest in BRCA1-deficient cells.
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Cell Line:SKOV3 and SKOV3-BRCA1-KD cells
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Concentration:2 μM
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Incubation Time:24 h
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Result:Showed particularly notable apoptosis induction effects in SKOV3 and SKOV3-BRCA1-KD cells.
Exhibited an even more striking effect on SKOV3 cells, inducing apoptosis in 25.7% of the population.
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Cell Line:SKOV3 and SKOV3-BRCA1-KD cells
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Concentration:1 μM
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Incubation Time:15 h
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Result:Decreased PARP-1 levels in SKOV3-BRCA1-KD cells.
Upregulated γH2AX levels particularly in BRCA1-deficient cancer cells.
Enhanced the pro-apoptotic protein Bax levels and suppressed the antiapoptotic protein Bcl-2 levels.
Downregulated NF-κB, TGF-β, Smad2, EGFR and E-cadherin levels.
Increased the expression of N-cadherin and vimentin.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c-nude mice using a cell-derived xenograft (CDX) SKOV3-BRCA1-KD tumor model[1]
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Dosage:2.5 mg/kg
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Administration:i.v. every three days for a total of six doses
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Result:Inhibited tumor growth by 71.70%.
Maintained stable body weights.
Showed no significant changes in any of these hematological parameters.
Exhibited a near-normal morphology, similar to that of the control group.
Reduced PARP-1 protein expression.
Chemical Information
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Molecular Weight 792.66
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Formula C25H46Cl2N6O6Pt
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SMILES
[NH3][Pt+4]([NH3])([O-]C(CN1C=NC(N(C(N2C)=O)C)=C1C2=O)=O)([O-]C(CCCCCCCCCCCCCCC)=O)([Cl-])[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
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Data Sheet (273 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)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Theophylline-platinum(IV) prodrug-1 Related Classifications
HY-175257 Related Classifications
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