Cetrelimab
Based on 1 Customer Validation
Cetrelimab (JNJ 63723283; JNJ 3283) is a human IgG4κ mAb targeting PD-1. Cetrelimab binds PD-1 (Kd=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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: ≥99.0%
- CAS No.: 2050478-92-5
- 분자량:144.76 kDa
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Human IgG4 kappa
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 Kd 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.; 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.
-
Animal Model:hPD-1KI model with mouse PD-1 ECD replaced by the human PD-1 ECD[1]
-
Dosage:10 mg/kg
-
Administration:Intraperitoneal injection; single dose at day 7 after tumor implantation
-
Result:hPD-1KI mice develop normally and have no immune abnormalities.
Significantly lowered tumor volume at Day 21.
-
Animal Model:Patient-derived xenograft (PDX) LG1306 lung model in mice[1]
-
Dosage:10 mg/kg
-
Administration:Intraperitoneal injection; every 5 days for 6 cycles
-
Result:Significantly reduced patient-derived tumor volume by 32%.
-
Animal Model:Good Laboratory Practice (GLP) toxicity study in cynomolgus[1]
-
Dosage:0, 10, 30, or 100 mg/kg
-
Administration:Intravenous injection; once weekly for 5 weeks
-
Result:Showed well tolerance in cynomolgus.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
-
Human IgG4 kappa
ELISA, FACS, Functional assay
-
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).
Chemical Information
-
CAS No. 2050478-92-5
-
Appearance Liquid
-
분자량 144.76 kDa
-
Color Colorless to light yellow
-
SMILES
[Cetrelimab]
-
Synonyms
JNJ 63723283; JNJ 3283
-
선적
Shipping with dry ice.
-
Formulation
Please refer to the lot-specific COA for specific buffer information.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
-
Data Sheet (262 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Inhibitory Antibodies User Guide (603 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)