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Dostarlimab (TSR-042) 是一种人源化抗 PD-1 单克隆抗体 |MedChemExpress

已有 538 次阅读 2024-9-3 09:44 |系统分类:科研笔记

MCE 国际站：Dostarlimab

CAS：2022215-59-2

品牌：MedChemExpress (MCE)

存储条件：Please store the product under the recommended conditions in the Certificate of Analysis.

生物活性：Dostarlimab (TSR-042) 是一种人源化抗 PD-1 单克隆抗体。Dostarlimab 与人 PD-1 具有高亲和力，并竞争性地抑制其与其配体 PD-L1 和 PD-L2 的相互作用，IC50s 分别为 1.8 nM 和 1.5 nM。

体外：Dostarlimab (10-10000 ng/mL) 以剂量依赖的方式与人和食蟹猴 CD3+ T 细胞上表达的原生 PD-1 受体结合[1]。 Dostarlimab (0-375 nM; 48 h) 在人 CD4+ T 细胞 MLR 实验中增加 IL-2 的产生，EC50 大约为 1 nM，在葡萄球菌肠毒素 B (SEB) 刺激的 PBMC 细胞中增加 IL-2 的产生，EC50 大约为 0.1 nM，增强干扰素 (IFN)-γ 的释放，EC50 大约为 0.5 nM[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内：Dostarlimab (200 µg/mouse; i.p.; twice weekly for 35 days) 在人源化小鼠模型中显示出抗肿瘤活性[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Humanized NOG-EXL mice, A549 and MDA-MB-436 tumor model[1] Dosage: 200 µg/mouse Administration: Intraperitoneal injection; twice weekly for 35 days Result: Resulted in great inhibition of tumor growth in an A549 lung cancer model (tumor growth inhibition [TGI] of 62% at termination). The antitumor activity was associated with a reduction in tumor-associated regulatory T cells and a trend toward increased tumor-infiltrating CD8+ T cells. Inhibited tumor growth of MDA-MB-436 breast cancer model (TGI of 53%). Clinical Trial

研究领域：Immunology/Inflammation

作用靶点：PD-1/PD-L1

参考文献：[1]. Kumar S, et al. Preclinical characterization of dostarlimab, a therapeutic anti-PD-1 antibody with potent activity to enhance immune function in in vitro cellular assays and in vivo animal models. MAbs. 2021 Jan-Dec;13(1):1954136.