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Sintilimab

MCE China：Sintilimab

Brand：MedChemExpress (MCE)

Cat. No.HY-P99048

CAS：2072873-06-2

Synonyms：IBI308

Purity：98.70%

Storage：Please store the product under the recommended conditions in the Certificate of Analysis.

Description：Sintilimab (IBI308) is a safe and effectivel humanized IgG4 monoclonal antibody that binds to PD-1 with a KD value of 74 pM. Sintilimab blocks the interaction of PD-1 with its ligands (PD-L1 and PL-L2), consequently helping to restore the endogenous antitumour T-cell response. Sintilimab combined with prebiotics inhibits tumor volume and regulates immune cell subpopulation balance in lung adenocarcinoma mice. Sintilimab can be used for the research of classical Hodgkin's lymphoma, non-small cell lung cancer and oesophageal cancer.

In Vitro：Sintilimab (12 h) shows a high level of PD-1 occupancy and has superior T cell activating characteristics in human peripheral blood mononuclear cells (PBMCs)[2]. Sintilimab (0.16-100 nM; 5 days) induces high secretion levels of IFN-γ and IL-2 in primary T cell assays[6].

In Vivo：Sintilimab (0.1 mg/kg, 1 mg/kg and 10 mg/kg, i.p., a single dose for 1, 8, 12, 15 days) shows antitumor effects against NCI-H292 tumors in a humanized mouse model[2]. Sintilimab (1 mg/kg, 3 mg/kg and 10 mg/kg, s.c., a single dose) demonstrates a high affinity for PD-1 molecules in NCI-H292 tumor-bearing NOG mice[2]. Sintilimab (20 mg/kg, i.p., once interval 2 days for 21 days) combined with prebiotics inhibits the volume of transplanted tumors in lung adenocarcinoma and alleviates the liver and kidney injury[4]. Pharmacokinetic parameters of Sintilimab (10 mg/kg, i.v., a single dose) in hPD-1 knock-in mouse[2] Parameter AUC0-4 (h·μg/mL) AUCinf (h·μg/mL) CL (mL/h) Cmax (μg/mL) T1/2 (h) Vss (mL) Sintilimab 6597.888 7846.554 0.025 218.519 35.623 1.262

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References：

[1]. Sheridan M Hoy. Sintilimab: First Global Approval Drugs. 2019 Feb;79(3):341-346.  [Content Brief]

[2]. Wang J, et al Durable blockade of PD-1 signaling links preclinical efficacy of sintilimab to its clinical benefit. MAbs. 2019 Nov-Dec;11(8):1443-1451.  [Content Brief]

[3]. Zhang L, et al. Sintilimab: A Promising Anti-Tumor PD-1 Antibody. Front Oncol. 2020 Nov 26;10:594558.  [Content Brief]

[4]. Yan Q, et al. Prebiotics Modulate Gut Microbiota-mediated T-cell Immunity to Enhance the Inhibitory Effect of Sintilimab in Lewis Lung Adenocarcinoma Model Mice. Anticancer Agents Med Chem. 2023;23(17):1966-1973.  [Content Brief]

[5]. Zhang L, et al. Sintilimab for the treatment of non-small cell lung cancer. Biomark Res. 2022 Apr 18;10(1):23.  [Content Brief]

[6]. Lou B, et al. Preclinical Characterization of GLS-010 (Zimberelimab), a Novel Fully Human Anti-PD-1 Therapeutic Monoclonal Antibody for Cancer. Front Oncol. 2021 Sep 15;11:736955.  [Content Brief]