耗材描述
Talacotuzumab
产品活性:Talacotuzumab (JNJ 56022473; CSL 362) 是一种 IgG1 型完全人源化的 CD123 中和单克隆抗体,含有修饰的 Fc 结构。Talacotuzumab 对 CD123、CD32b/c、CD16-158F、CD16-158V 的 KD 分别为 0.43 nM、188 nM、46 nM、16.8 nM。Talacotuzumab 抑制 IL-3 与 CD123 的结合,从而拮抗靶细胞中的 IL-3 信号传导。Talacotuzumab 使 Fc 区发生突变以增加对 CD16 (FcγRIIIa) 的亲和力,从而增强抗体依赖性细胞介导的细胞毒性 (ADCC)。Talacotuzumab 在体内非常有效地减少急性髓性白血病 (AML) 异种移植小鼠模型中的白血病细胞生长。
产品来源: https://www.medchemexpress.cn/talacotuzumab.html
研究领域:Immunology/Inflammation
作用靶点:Interleukin Related
In Vitro: Talacotuzumab (JNJ 56022473; CSL 362) strongly mediates ADCC of TF-1 cells with an ic50 of 5 ng/ml (33 pM).
Talacotuzumab (1 μg/ml; pretreatment for 24 hours) inhibits TLR7-stimulated (Imiquimod; HY-B0180; 0.5 μM; for 6 days) and TLR9-stimulated (CpG C; 0.5 μM; for 6 days) IFN-α production in both SLE donors and healthy donors plasmacytoid dendritic cells (pDCs) and basophils, whereas TLR4-stimulated (LPS; HY-D1056; 10 μg/ml) production is not significantly reduced. Talacotuzumab inhibits TLR7- and TLR9-induced plasmablast expansion and proliferation by depletion of plasmacytoid dendritic cells (pDCs).
In Vivo: Talacotuzumab (JNJ 56022473; CSL 362; 300 μg; ip; thrice weekly for 5 weeks) results in a significant delay in tumor growth compared with an isotype control in acute myeloid leukaemia mice xenografts.
Talacotuzumab (1, 10, 30 mg/kg; s.c.; single injection) has maximal serum concentrations at 48 hours of ~12, 190, and 380 μg/ml at doses of 1, 10, and 30 mg/kg in naive cynomolgus monkeys, respectively.
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