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编 号：F756160
分子式：C46H46N6O5
分子量：762.89
分子式：C46H46N6O5
分子量：762.89
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CAS No: 2820286-56-2
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生物活性：
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.
体内研究：
T-PBA (1-10 mg/kg; i.v.; every 3 days for 4 times) could significantly delay tumor growth in two Her2-positive xenograft models in mice without obvious toxicity and side effects, and the effect is better than Trastuzumab.Animal Model:Female balb/c nude mice, SKOV3 and NCI-N87 tumor model
Dosage:1, 5 and 10 mg/kg
Administration:Tail vein injection on days 0, 3, 6, and 9
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.
体外研究：
Anticancer agent 81 (Compound 37b3) (72 h) shows cytotoxicity against SKOV3, MDA-MB-231 and NCI-N87 cells.Anticancer agent 81 (0-5 μM) induces DNA interstrand cross-linking.Anticancer agent 81 (0-3 nM; 24 h) arrests SKOV3 cell cycle at the S-phase.Anticancer agent 81 (0-3 nM; 48 h) induces SKOV3 cell apoptosis.Anticancer agent 81 (25 nM; 12 h) acts on DNA in the nucleus after entering SKOV3 cells and MDA-MB-231 cells.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.Anticancer agent 81 covalently binds to the DNA sequences and acts on the major groove of DNA.
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.
体内研究：
T-PBA (1-10 mg/kg; i.v.; every 3 days for 4 times) could significantly delay tumor growth in two Her2-positive xenograft models in mice without obvious toxicity and side effects, and the effect is better than Trastuzumab.Animal Model:Female balb/c nude mice, SKOV3 and NCI-N87 tumor model
Dosage:1, 5 and 10 mg/kg
Administration:Tail vein injection on days 0, 3, 6, and 9
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.
体外研究：
Anticancer agent 81 (Compound 37b3) (72 h) shows cytotoxicity against SKOV3, MDA-MB-231 and NCI-N87 cells.Anticancer agent 81 (0-5 μM) induces DNA interstrand cross-linking.Anticancer agent 81 (0-3 nM; 24 h) arrests SKOV3 cell cycle at the S-phase.Anticancer agent 81 (0-3 nM; 48 h) induces SKOV3 cell apoptosis.Anticancer agent 81 (25 nM; 12 h) acts on DNA in the nucleus after entering SKOV3 cells and MDA-MB-231 cells.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.Anticancer agent 81 covalently binds to the DNA sequences and acts on the major groove of DNA.
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