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1mg | ||
5mg | ||
10mg | ||
Other Sizes |
Targets |
PD-1/PD-L1, PD-1/PD-L2, IFN-γ, IL-2, and TNF-α[1]
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ln Vitro |
Cetrelimab (0.01-30 nM; 5 d) binds to endogenous PD-1 on activated CD4+ and CD8+ T cells with EC50s of 0.17-0.22 µg/mL and 0.16-0.22 µg/mL, respectively[1]. In Jurkat-PD-1 NFAT reporter cells expressing PD-L1, cetrelimab (0.01-30 μg/mL; 24 h) reverses PD-1-mediated inhibition of TCR signaling[1]. With EC50s of 0.08 ng/mL, 0.07 ng/mL, and 0.02 ng/mL, respectively, cetrelimab (0.001-100 nM; 6 d) raises IFN-γ, IL-2, and TNF-α. With a Kd value of 0.9 nM, cetrelimab binds to PD-1 in cynomolgus [1].
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ln Vivo |
Cetrelimab (10 mg/kg; ip; single dose) reduces the volume of tumors in PD-1 knock-in (hPD-1KI) mice harboring MC38 tumors and exhibits antitumor efficaciousness[1]. In a patient-derived xenograft (PDX) lung model in mice, cetrelimab (10 mg/kg; ip; once every 5 days for 30 d) significantly increases peripheral blood CD8+ T cells[1]. In the cynomolgus model, cetrelimab (10–100 mg/kg; iv; once weekly for 5 weeks) has good tolerance[1]. Target-mediated drug deposition (TMDD) may be the cause of cetrelimab's nonlinear pharmacokinetics (PK) in cynomolgus (0.1–10 mg/kg; IV; single dose, monitored for 57 d)[1].
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Animal Protocol |
Animal/Disease Models: hPD-1KI model with mouse PD-1 ECD replaced by the human PD-1 ECD[1]
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip)injection; single dose at day 7 after tumor implantation Experimental Results: hPD-1KI mice develop normally and have no immune abnormalities. Dramatically lowered tumor volume at Day 21. Animal/Disease Models: Patient-derived xenograft (PDX) LG1306 lung model in mice [1] Doses: 10 mg/kg Route of Administration: intraperitoneal (ip)injection; every 5 days for 6 cycles Experimental Results: Dramatically diminished patient-derived tumor volume by 32%. Animal/Disease Models: Good Laboratory Practice (GLP) toxicity study in cynomolgus[1] Doses: 0, 10, 30, or 100 mg/kg Route of Administration: intravenous (iv)injection; once weekly for 5 weeks Experimental Results: demonstrated well tolerance in cynomolgus. |
References |
[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.
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CAS # |
2050478-92-5
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.