Cetrelimab  (Synonyms: JNJ 63723283; JNJ 3283)

Cetrelimab (JNJ 63723283; JNJ 3283) is a human IgG4κ mAb targeting PD-1. Cetrelimab binds PD-1 (K_d=1.72 nM, HEK293) to block the interaction of PD-1 with PD-L1 and PD-L2 (IC₅₀s=111.7 ng/mL and 138.6 ng/mL, respectively). Cetrelimab stimulates peripheral T cells, increases IFN-γ, IL-2, TNF-α level and inhibits tumor growth in vivo^[1].

Human IgG4 kappa

Human IgG4 (S228P) kappa, Isotype Control

Human

PDCD1/PD-1/CD279

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^[1].
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^[1].
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^[1].
Cetrelimab binds to PD-1 in cynomolgus with a K_d value of 0.9 nM^[1].

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

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^[1].
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^[1].
Cetrelimab (10-100 mg/kg; i.v.; once weekly for 5 weeks) has well tolerance in cynomolgus model^[1].
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)^[1].

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

5133  [NCBI]

Q15116

ELISA, FACS, Functional assay

Unconjugated

The product can be reconstituted/diluted with sterile PBS or saline.

144.76 kDa

2050478-92-5

Liquid

Colorless to light yellow

[Cetrelimab]

Shipping with dry ice.

Please refer to the lot-specific COA for specific buffer information.

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

• 
  Human IgG4 kappa

• 
  Immobilized Human PD-1 Protein (ECD, His Tag) can bind Cetrelimab. The EC₅₀ for this effect is 5.75 ng/mL.
• 
  Flow cytometric analysis of 1X10⁶ 10 ng/mL PMA and 1 μg/mL Ionomycin co-stimulated Jurkat cells(24h) labeling Cetrelimab (HY-P99499, red). Cells were fixed with 4% paraformaldehyde. Then stained with the primary antibody at 1/200 dilution for an hour at 4℃. Alexa Fluor 488-conjugated AffiniPure Goat Anti-Human IgG H&L (HY-P83776) was used as the secondary antibody at 1/1,000 dilution for 30 minutes at 4℃. Human IgG4 kappa (HY-P99003, blue) was used as the isotype control, cells without incubation with primary antibody were used as the unlabeled control (black).

• [1]. DeAngelis N, et al. Discovery and pharmacological characterization of cetrelimab (JNJ-63723283), an anti-programmed cell death protein-1 (PD-1) antibody, in human cancer models. Cancer Chemother Pharmacol. 2022 Apr;89(4):515-527.  [Content Brief]