Anticancer agent 81
Anticancer agent 81 (Compound 37b3) is an anticancer agent and can induce tumor cell cycle arrest and apoptosis. Anticancer agent 81 can be used as a payload to conjugate with Trastuzumab (HY-P9907) to obtain the antibody–agent conjugate (ADC) T-PBA. T-PBA maintained its mode of target and internalization ability of Trastuzumab.
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- No. CAS: 2820286-56-2
- Fòrmula: C46H46N6O5
- Peso molecular:762.89
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Actividad biológica
Anticancer agent 81 (Compound 37b3) (72 h) shows cytotoxicity against SKOV3, MDA-MB-231 and NCI-N87 cells[1].
Anticancer agent 81 (0-5 μM) induces DNA interstrand cross-linking[1].
Anticancer agent 81 (0-3 nM; 24 h) arrests SKOV3 cell cycle at the S-phase[1].
Anticancer agent 81 (0-3 nM; 48 h) induces SKOV3 cell apoptosis[1].
Anticancer agent 81 (25 nM; 12 h) acts on DNA in the nucleus after entering SKOV3 cells and MDA-MB-231 cells[1].
Anticancer agent 81 induces DDR signaling pathways via cross-linking DNA and then activates the caspase cascade and PARP, finally leading to cell cycle arrest and apoptosis[1].
Anticancer agent 81 covalently binds to the DNA sequences and acts on the major groove of DNA[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SKOV3, MDA-MB-231 and NCI-N87
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Concentration:
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Incubation Time:72 h
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Result:Showed cytotoxicity with IC50s of 0.17 ± 0.07, 0.90 ± 0.11 and 0.94 ± 0.14 nM against SKOV3, MDA-MB-231 and NCI-N87 cells, respectively.
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Cell Line:SKOV3
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Concentration:0.33, 1 and 3 nM
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Incubation Time:24 h
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Result:Inhibited the cell cycle at the S-phase.
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Cell Line:SKOV3
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Concentration:0.33, 1 and 3 nM
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Incubation Time:48 h
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Result:Induced cell apoptosis in a concentration-dependent manner.
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Cell Line:SKOV3 and NCI-N87
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Concentration:0.02, 0.1, 0.5, 2.5 and 12.5 nM
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Incubation Time:48 h
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Result:Induced the phosphorylation of histone 2AX (γ-H2AX) in a dose-dependent manner. Induced the cleavage of PARP (cPARP) and caspase 3 (cCas3) in a concentration-dependent manner.
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, SKOV3 and NCI-N87 tumor model[1]
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Dosage:1, 5 and 10 mg/kg
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Administration:Tail vein injection on days 0, 3, 6, and 9
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Result:Inhibited tumor growth in a dose-dependent manner (57.5% inhibition at 1 mg/kg, 70.0% inhibition at 5 mg/kg, and 91.5% inhibition at 10 mg/kg in SKOV3 tumor model; the tumor growth inhibitory rate was 50.2% for 1 mg/kg, 88.0% for 5 mg/kg, and 97.1% for 10 mg/kg in NCI-N87 tumor model) without obvious side effects.
Chemical Information
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No. CAS 2820286-56-2
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Peso molecular 762.89
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Fòrmula C46H46N6O5
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SMILES
O=C1N(CCN2CCN(CCCCCOC3=C(OC)C=C4C(N=C[C@@](CC(C5=CC=C(N)C=C5)=C6)([H])N6C4=O)=C3)CC2)C(C7=CC=CC8=CC9=CC=CC=C9C1=C78)=O
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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)
Anticancer agent 81 Related Classifications
HY-151207 Related Classifications
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