Size | Price | |
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1mg | ||
5mg | ||
Other Sizes |
Targets |
CD40 0.3 nM (IC50)
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ln Vitro |
Primary monocyte-derived dendritic cells (moDCs) produce less TNF in response to rCD154 when iscalimab (0.01–1 μg/mL, overnight) is used, with an IC50 of 0.04 μg/mL [3]. With IC50 values of 0.02, 0.03, and 0.01 μg/mL, respectively, iscalimab (3 days) suppresses the proliferation of human, rhesus, and cynomolgus monkey PBMC stimulated by rCD154 [3]. With an EC50 value of roughly 0.2 μg/mL, iscalimab binds CD40 on B lymphocytes from humans, rhesus monkeys, and cynomolgus monkeys [3]. B cells internalize iscalimab (2 μg/mL, 3 h) in a CD40-dependent manner [3].
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ln Vivo |
In rhesus monkeys, iscalimab (150 mg/kg/week, subcutaneously administered for 13 weeks) was well tolerated and did not result in any dose-limiting toxicities [3]. In rhesus monkeys, iscalimab (10 mg/kg, intravenously) totally suppresses T cell-dependent antibody responses [3]. Cynomolgus monkeys receiving kidney transplants have longer allograft survival when given iscalimab (30 mg/kg intravenously) [4].
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Cell Assay |
Cell Viability Assay[3]
Cell Types: PBMCs from humans, rhesus and cynomolgus animals Tested Concentrations: 0-1 μg/mL approximately Incubation Duration: 3 days Experimental Results: Inhibited rCD154-induced proliferation of PBMCs with IC50s of 0.02, 0.03, and 0.01 μg/mL, respectively. |
Animal Protocol |
Animal/Disease Models: Kidney transplant cynomolgus[4]
Doses: 30 mg/kg Route of Administration: iv Experimental Results: Prolonged allograft survival. Well-tolerated with no evidence of thromboembolic events or CD40 pathway activation. |
References |
[1]. Kahaly GJ, et al. A Novel Anti-CD40 Monoclonal Antibody, Iscalimab, for Control of Graves Hyperthyroidism-A Proof-of-Concept Trial. J Clin Endocrinol Metab. 2020 Mar 1;105(3):dgz013.
[2]. Flandre TD, et al. Immunosuppression Profile of CFZ533 (Iscalimab), a Non-Depleting Anti-CD40 Antibody, and the Presence of Opportunistic Infections in a Rhesus Monkey Toxicology Study. Toxicol Pathol. 2022 Jul;50(5):712-724. [3]. Ristov J, et al. Characterization of the in vitro and in vivo properties of CFZ533, a blocking and non-depleting anti-CD40 monoclonal antibody. Am J Transplant. 2018 Dec;18(12):2895-2904. [4]. Cordoba F, et al. A novel, blocking, Fc-silent anti-CD40 monoclonal antibody prolongs nonhuman primate renal allograft survival in the absence of B cell depletion. Am J Transplant. 2015 Nov;15(11):2825-36. |
CAS # |
2031153-61-2
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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.