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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[1]. | [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[1]. Animal Model: | Female balb/c nude mice, SKOV3 and NCI-N87 tumor model[1] | 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. |
| [References]
[1] Lai W, et al. Design, Synthesis, and Bioevaluation of a Novel Hybrid Molecular Pyrrolobenzodiazepine-Anthracenecarboxyimide as a Payload for Antibody-Drug Conjugate. J Med Chem. 2022 Aug 18. DOI:10.1021/acs.jmedchem.2c00471 |
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