DPAP
DPAP is a p-ERK1/2 inhibitor with an IC50 of 7.85 μM against p-ERK1/2. DPAP inhibits the expression of p-MEK1/2 and disrupts the Ras-ERK signaling pathway. DPAP inhibits the expression of COX-2 in nerve cells. DPAP damages DNA and mitochondria, induces Apoptosis via the mitochondrial pathway, and upregulates PD-L1. DPAP inhibits melanoma metastasis and angiogenesis, and inactivates spinal microglia and astrocytes. DPAP exhibits anti-melanoma activity and can be combined with anti-PD-1 monoclonal antibodies to modify anti-tumor effects. DPAP is applicable for the research of melanoma.
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- Fòrmula: C22H28Cl2N2O10Pt
- Peso molecular:746.46
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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COX-2 |
The cellular uptake of DPAP (2 μM; 72 h) in A375 melanoma cells is 2.53-fold higher than that of CDDP[1].
DPAP (72 h) inhibits the proliferation of melanoma A375 cells, mouse melanoma B16-F10 cells, and normal renal HK-2 cells. After 72 h of incubation, its IC50 values are 8.05 μM, 5.96 μM, and 35.12 μM, respectively, indicating selective cytotoxicity against cancer cells[1].
DPAP (1-8 μM; 72 h) increases the level of DNA-bound Pt in A375 melanoma cells; at 8 μM for 72 h, it upregulates the expression of γ-H2AX, indicating the presence of DNA damage[1].
DPAP (8 μM; 48 h) induces S-phase cell cycle arrest in melanoma A375 cells[1].
DPAP (8 μM; 72 h) regulates the expression of apoptosis-related proteins (upregulating Cyt c and Bax, downregulating Bcl-2) and induces late apoptosis in human melanoma A375 cells[1].
DPAP (8 μM; 72 h) regulates the Ras-ERK signaling pathway in melanoma A375 cells[1].
DPAP (8 μM; 24 h) downregulates the expressions of p-ERK1/2 and COX-2, but does not alter the expression of NF-L, in HT22 mouse hippocampal neuronal cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A375 cells
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Concentration:8 μM
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Incubation Time:48 h
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Result:Arrested A375 cells primarily in the S phase, similar to CDDP, indicating inhibition of DNA synthesis.
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Cell Line:A375 cells
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Concentration:8 μM
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Incubation Time:72 h
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Result:Significantly downregulated p-MEK1/2 and p-ERK1/2 expression relative to control cells, while having only slight effects on NRAS, MEK1/2, and ERK1/2 expression.
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Cell Line:HT22 cells
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Concentration:8 μM
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Incubation Time:24 h
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Result:Suppressed p-ERK1/2 and COX-2 expression in HT22 cells relative to control cells, and did not affect NF-L expression, unlike CDDP which reduced NF-L levels.
DPAP (1.5 mg Pt kg−1; intravenous injection; once every 2 days; for 1 week) inhibits the activation of microglia and astrocytes in the spinal dorsal horn of melanoma-bearing mice, demonstrating potential to alleviate cancer pain-related central sensitization[1].
Combination treatment with DPAP (2.5 mg Pt kg-1; intravenous injection; once every 2 days; for 2 consecutive weeks) and anti-PD-1 mAb (12.5 mg kg-1; intravenous injection; administered on days 4, 9 and 14) synergistically enhances the anti-melanoma efficacy[1].
DPAP (10-40 mg kg-1; intravenous injection; once every 2 days) exhibits a high median lethal dose of 33.60 mg kg-1 and favorable biocompatibility in healthy female C57BL/6 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (female, 6−8 weeks old, 18−20 g, subcutaneous inoculation of murine B16−F10 melanoma cells, tumors grown to ~50 mm3)[1]
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Dosage:1.5 mg Pt kg-1
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Administration:i.v.; once every 2 days; 15 days
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Result:Reduced average tumor weight to 0.10 g, compared to 1.19 g in the PBS control group.
Reduced average tumor volume to 412.11 mm3, compared to 1539.47 mm3 in the PBS control group.
Caused no significant change in mouse body weight relative to the PBS group.
Showed no apparent alterations in heart, liver, spleen, lung, and kidney tissues via histological examination.
Significantly reduced the fluorescence intensity of p-ERK1/2 in tumor tissue.
Significantly weakened the fluorescence intensity of VEGF-A in tumor tissue.
Chemical Information
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Peso molecular 746.46
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Fòrmula C22H28Cl2N2O10Pt
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SMILES
COC1=CC(OCC(O[Pt](Cl)(Cl)(OC(COC2=C(C(C)=O)C=CC(OC)=C2)=O)([NH3])[NH3])=O)=C(C(C)=O)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DPAP Related Classifications
HY-182899 Related Classifications
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