Iscalimab
Iscalimab (CFZ-533) is a non-depleting IGg1 monoclonal antibody targeting CD40 (KD: 0.3 nM). The Fc region of Iscalimab incorporates the N297A mutation, designed to remove the N-glycosylation site in the CH2 domain and thereby attenuate or eliminate the antibody's ADCC effector function. Iscalimab can be used for research of Graves' hyperthyroidism and autoimmune diseases.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
IC50 & Target
TNFRSF5/CD40
In Vitro
Iscalimab (0.01-1 μg/mL, overnight) blocks rCD154-induced TNF production by primary monocyte-derived dendritic cells (moDCs), with an IC50 of 0.04 μg/mL[3].
Iscalimab (3 days) inhibits rCD154-induced proliferation of PBMCs from humans, rhesus and cynomolgus animals with IC50s of 0.02, 0.03, and 0.01 μg/mL, respectively[3].
Iscalimab bind CD40 on B cells from humans, rhesus and cynomolgus animals with EC50 values of approximately 0.2 μg/mL[3].
Iscalimab (2 μg/mL, 3 h) is internalized by B cells in a CD40-dependent manner[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PBMCs from humans, rhesus and cynomolgus animals
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Concentration:0-1 μg/mL approximately
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Incubation Time:3 days
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Result:Inhibited rCD154-induced proliferation of PBMCs with IC50s of 0.02, 0.03, and 0.01 μg/mL, respectively.
In Vivo
Iscalimab (10 mg/kg, i.v.) completely inhibits T cell-dependent antibody response in Rhesus monkeys[3].
Iscalimab (30 mg/kg, i.v.) prolongs allograft survival in kidney transplant cynomolgus[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Kidney transplant cynomolgus[4]
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Dosage:30 mg/kg
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Administration:i.v.
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Result:Prolonged allograft survival.
Well-tolerated with no evidence of thromboembolic events or CD40 pathway activation.
Chemical Information
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SMILES
[Iscalimab]
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Synonyms
CFZ-533; OM11-62MF
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Iscalimab Related Classifications
HY-P99670A Related Classifications
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