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MCE 国际站：Anticancer agent 81
产品活性：Anticancer agent 81 (Compound 37b3) 是一种抗癌剂，能诱导肿瘤细胞周期阻滞和凋亡 (apoptosis)。Anticancer agent 81 可作为有效载荷与 Trastuzumab (HY-P9907) 结合得→到抗体偶联药物 (ADC) T-PBA。T-PBA 维持了 Trastuzumab 的靶向模式和内化能力。
研究领域：Apoptosis | Antibody-drug Conjugate/ADC Related
作用靶点：Apoptosis | ADC Cytotoxin
In Vitro: 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.
In Vivo: 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.
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