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Nivolumab
CAS No. : 946414-94-4
MCE 国际站:Nivolumab
产品活性:Nivolumab 是一种 PD-1 人源类 IgG4 抗体类抑制剂,用于晚期(转移性)非小细胞肺癌的研究。
作用靶点:PD-1/PD-L1
In Vitro: Nivolumab binds to CHO cells expressing PD-1 with an EC50 of 1.66 nM, but does not bind to the parental CHO cell line. Nivolumab binds to PD-1 on activated T cells with an EC50 of 0.64 nM. Nivolumab also inhibits the interaction between PD-1 and its ligands, PD-L1 and PD-L2, with IC50 values of 2.52 and 2.59 nM, respectively. Nivolumab (1.5 ng/mL) can enhance T-cell reactivity in the presence of a T-cell receptor stimulus.
In Vivo: Nivolumab (10 and 50 mg/kg, i.v.) is well tolerated in cynomolgus monkeys. Serum chemistry changes are limited to a reversible 28% decrease in T3 at week 13 in females treated with 50 mg/kg. T4 and TSH levels are unchanged. In males treated with 50 mg/kg, there are no changes in T3, T4, or TSH levels. Nivolumab exposure increases in an approximately dose-proportional manner between 10 and 50 mg/kg, with no substantial sex differences noted.
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