Cetrelimab 产品活性：Cetrelimab (JNJ 63723283; JNJ 3283) 是一种靶向 PD-1 的人源 IgG4κ 单克隆抗体。Cetrelimab 结合 PD-1 的 Kd 为 1.72 nM (HEK293 细胞)。由此，Cetrelimab 阻断 PD-1 与 PD-L1 和 PD-L2 的相互作用 (IC50 分别为 111.7 ng/mL 和 138.6 ng/mL)。Cetrelimab 还刺激外周 T 细胞，增加细胞因子 (IFN-γ, IL-2, TNF-α) 水平，并抑制体内肿瘤生长。 产品来源： https://www.medchemexpress.cn/cetrelimab.html 研究领域：Immunology/Inflammation | Apoptosis 作用靶点：PD-1/PD-L1 | Interleukin Related | TNF Receptor In Vitro: Cetrelimab (0.01-30 nM; 5 d) binds to endogenous PD-1 on activated CD4+ and CD8+ T cells with EC50s of 0.16-0.22 µg/mL and 0.17-0.22 µg/mL, respectively. Cetrelimab (0.01-30 μg/mL; 24 h) reverse PD-1-mediated suppression of TCR signaling in Jurkat-PD-1 NFAT reporter cells with CHO-K1 expressing PD-L1. Cetrelimab (0.001-100 nM; 6 d) increases IFN-γ, IL-2, and TNF-α with EC50s of 0.08 ng/mL, 0.07 ng/mL, and 0.02 ng/mL, respectively. Cetrelimab binds to PD-1 in cynomolgus with a Kd value of 0.9 nM. In Vivo: Cetrelimab (10 mg/kg; i.p.; single dose) has antitumor efficacy, and decreases tumor volume in PD-1 knock-in (hPD-1KI) mice with MC38 tumor. Cetrelimab (10 mg/kg; i.p.; once every 5 days for 30 d) results significant increases in peripheral blood CD8+ T cells in patient-derived xenograft (PDX) lung model in mice. Cetrelimab (10-100 mg/kg; i.v.; once weekly for 5 weeks) has well tolerance in cynomolgus model. Cetrelimab (0.1-10 mg/kg; i.v.; single dose, monitored for 57 d) shows an nonlinear pharmacokinetics (PK) in cynomolgus, possibly attributable to target-mediated drug deposition (TMDD). 相关产品：Resatorvid | Disulfiram | Polyinosinic-polycytidylic acid | Raleukin | Deucravacitinib | Shikonin | Atezolizumab | Pembrolizumab | Infliximab | Cilengitide | Dupilumab | Tocilizumab | Nivolumab | Apilimod | Fisetin | BMS-1 | Oxidopamine hydrobromide | BMS-202 | Adalimumab | Anti-Mouse PD-1 Antibody (RMP1-14) | Etanercept | JQ-1 (carboxylic acid) | Anti-Mouse PD-L1/B7-H1 Antibody (10F.9G2) | N-Formyl-Met-Leu-Phe | Durvalumab | LMT-28 | Tomivosertib | Apremilast | R-7050 品牌介绍: MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供最新最全的高品质小分子活性化合物；10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；设有专业的实验中心和严格的质控、验证体系；提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；产品的生物活性多经各国客户实验验证；Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；与世界各大制药公司及知名科研机构建立了长期的合作。