1. Immunology/Inflammation
  2. PD-1/PD-L1
  3. Sintilimab

Sintilimab  (Synonyms: IBI308)

Cat. No.: HY-P99048 Purity: 98.70%
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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.

For research use only. We do not sell to patients.

CAS No. : 2072873-06-2

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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[1][2][3][4][5].

In Vitro

Sintilimab (150 ng/μL, 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]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NOG mice reconstituted with human PBMCs[2]
Dosage: 1 mg/kg, 3 mg/kg and 10 mg/kg
Administration: i.p., a single dose at 24 h and 72 h
Result: Dose-dependently showed a higher percentage of PD-1 molecule occupancy compared with MDX-1106 (HY-P9903) and MK-3475 (HY-P9902) in mice.
Animal Model: NCI-H292 tumor-bearing NOG mice[2]
Dosage: 1 mg/kg, 3 mg/kg and 10 mg/kg
Administration: s.c., a single dose at 24 h
Result: Increased PD-1 receptor occupancy in both peripheral and CD3+ tumor-infiltrating T cells (TILs) to more than 90% in NCI-H292 tumor-bearing mice.
Animal Model: NCI-H292 tumors in a humanized xenograft mouse model[2]
Dosage: 0.1 mg/kg, 1 mg/kg and 10 mg/kg
Administration: i.p., a single dose at day 1, 8, 12, 15
Result: Inhibited tumor growth much more effectively and was significantly higher in the ratio of CD8+ to Treg tumor-infiltrating lymphocytes than MDX-1106 (HY-P9903) and MK-3475 (HY-P9902) in mice.
Animal Model: C57BL/6J mice (6-8 weeks old, body mass 20-25 g) with lung adenocarcinoma[4]
Dosage: 20 mg/kg
Administration: i.p., once interval 2 days for 21 days
Result: Significantly decreased the tumor volume, showed blurred cell structure and mildly damaged liver lobules and reduced liver and kidney injury in lung adenocarcinoma mice.
Clinical Trial
CAS No.
Appearance

Liquid

Color

Colorless to light yellow

SMILES

[Sintilimab]

Storage

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

Format
  • Human IgG4 kappa
Purity & Documentation

Purity: 98.70%

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