anti-TNBC agent-15
anti-TNBC agent-15 is a platinum (IV) complex with anti-triple-negative breast cancer activity. anti-TNBC agent-15 inhibits cancer cell viability. anti-TNBC agent-15 reverses the resistance of triple-negative breast cancer cells to Cisplatin (HY-17394), increases intracellular uptake, and effectively triggers apoptosis by inducing DNA damage, enhancing intracellular ROS accumulation and activating the mitochondrial pathway. anti-TNBC agent-15 enhances lipid peroxidation, interferes with the signal transduction of the cystine/glutamate transporter-glutathione peroxidase axis, and induces ferroptosis. anti-TNBC agent-15 significantly inhibits tumor growth in triple-negative breast cancer/Cisplatin xenograft models. anti-TNBC agent-15 can be used for the research of triple-negative breast cancer.
For research use only. We do not sell to patients.
- Formula: C34H39ClN6O13PtS
- Molecular Weight:1002.31
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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
anti-TNBC agent-15 (Compound 14) (100 nM-50 μM; 72 h) potently inhibits MDA-MB-231, A549, HCT-116, A549/CDDP, MDA-MB-231/CDDP and MCF-10 A cells, with IC50 values of 2.38, 3.77, 4.36, 4.29, 2.25 and 12.17, respectively[1].
anti-TNBC agent-15 (5 μM; 12-24 h) significantly increases intracellular platinum accumulation in MDA-MB-231 cells and cisplatin-resistant MDA-MB-231/CDDP cells, potently induces DNA damage in MDA-MB-231/CDDP cells, and elevates the expression levels of γ-H2AX and p53 as well as the olive tail moment value in the comet assay[1].
anti-TNBC agent-15 (5 μM; 24 h) induces apoptosis in Cisplatin-resistant MDA-MB-231/CDDP cells by upregulating pro-apoptotic proteins and downregulating the anti-apoptotic protein Bcl-2, and disrupts the mitochondrial membrane potential of the cells[1].
anti-TNBC agent-15 (5 μM; 24 h) inhibits the cystine/glutamate transporter-glutathione peroxidase axis in Cisplatin-resistant MDA-MB-231/CDDP cells by downregulating the expression of xCT and GPX4[1].
anti-TNBC agent-15 (5 μM; 24-72 h) induces cell death in cisplatin-resistant MDA-MB-231/CDDP cells via ferroptosis[1].
anti-TNBC agent-15 (5 μM; 12-24 h) disrupts the GSH redox system and induces extensive lipid peroxidation in Cisplatin-resistant MDA-MB-231/CDDP cells[1].
anti-TNBC agent-15 (5 μM; 24 h) inhibits migration and invasion of cisplatin-resistant MDA-MB-231/CDDP cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231, A549, HCT-116, A549/CDDP, MDA-MB-231/CDDP, MCF-10 A cells
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Concentration:100 nM, 500 nM, 1 μM, 5 μM, 10 μM, 50
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Incubation Time:72 h
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Result:Exhibited the highest cytotoxicity across all tested cell lines, with IC50 values of 2.38 μM (MDA-MB-231), 3.77 μM (A549), 4.36 μM (HCT-116), 4.29 μM (A549/CDDP), 2.25 μM (MDA-MB-231/CDDP), and 12.17 μM (MCF-10 A).
Showed a resistance factor (RF1) of 1.14 (A549/CDDP vs A549) and RF2 of 0.95 (MDA-MB-231/CDDP vs MDA-MB-231), and a selectivity factor (SF) of 5.11 (MCF-10 A vs MDA-MB-231).
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Cell Line:MDA-MB-231/CDDP cells
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Concentration:5 μM
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Incubation Time:24 h
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Result:Induced an apoptotic rate of 52.87% in MDA-MB-231/CDDP cells, which was higher than the rates induced by ligand 8 (22.95%), oxaliplatin (38.4%), and the combination of ligand 8 and oxaliplatin (46.23%).
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Cell Line:MDA-MB-231/CDDP cells
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Concentration:5 μM
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Incubation Time:24 h
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Result:Upregulated the expression of pro-apoptotic proteins Cyt c, Bax, cleaved caspase 3, and cleaved caspase 9, with protein densities relative to β-actin reaching ~0.5, ~0.75, ~0.85, and ~0.7, respectively.
Downregulated the expression of anti-apoptotic protein Bcl-2, with a protein density relative to β-actin of ~0.05.\nSignificantly downregulated the expression of cystine/glutamate transporter (xCT) and glutathione peroxidase 4 (GPX4) proteins, with protein densities relative to β-actin reaching ~0.3 and ~0.1, respectively.
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Cell Line:MDA-MB-231/CDDP cells
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Concentration:5 μM
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Incubation Time:24 h
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Result:Inhibited the migration and invasion of Cisplatin-resistant MDA-MB-231/CDDP cells
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c-nude (female)[1]
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Dosage:5.0 mg/kg; 16.7 mg/kg
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Administration:i.v.; every 7 days; 28 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 44.6% at 5.0 mg/kg.
Achieved a tumor growth inhibition (TGI) rate of 63.4% at 16.7 mg/kg.
Showed no significant body weight differences compared to saline control during 28-day treatment, indicating low systemic toxicity.
Induced extensive cell nuclear loss in tumors (16.7 mg/kg dose group, H&E staining).
Demonstrated reduced proliferative activity in tumors (16.7 mg/kg dose group, Ki-67 staining).
Chemical Information
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Molecular Weight 1002.31
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Formula C34H39ClN6O13PtS
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SMILES
O=C(O[Pt](OC1=O)([NH2][C@H]2[C@H]3CCCC2)([NH2]3)(Cl)OC1=O)CCCC(OCCOC4=CC=C(/N=N/C5=CC=C(S(=O)(NC6=NC=CC=C6)=O)C=C5)C=C4C(OC)=O)=O
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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)
anti-TNBC agent-15 Related Classifications
HY-182067 Related Classifications
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