Evobrutinib (M-2951, MSC-2364447C) is a highly selective BTK inhibitor with an IC50 of 37.9 nM. It has potential anti-neoplastic activity.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Tyrosine-protein kinase BTK inhibitor
Product Description
Information
Evobrutinib (M-2951) Evobrutinib (M-2951, MSC-2364447C) is a highly selective BTK inhibitor with an IC50 of 37.9 nM. It has potential anti-neoplastic activity.
Targets
BTK (Cell-free assay) 37.9 nM
In vitro
Evobrutinib can inhibit the activity of BTK and prevent the activation of the BCR signaling pathway. It is metabolized via hydroxylation, hydrolysis, O-dealkylation, glucuronidation, and GSH conjugation.
1.Haselmayer P, Camps M, Liu-Bujalski L, Nguyen N, Morandi F, Head J, O'Mahony A, Zimmerli SC, Bruns L, Bender AT et al.. (2019) Efficacy and Pharmacodynamic Modeling of the BTK Inhibitor Evobrutinib in Autoimmune Disease Models.. J Immunol, 202 (10):(2888-2906). [PMID:30988116]
2.Montalban X, Arnold DL, Weber MS, Staikov I, Piasecka-Stryczynska K, Willmer J, Martin EC, Dangond F, Syed S, Wolinsky JS et al.. (2019) Placebo-Controlled Trial of an Oral BTK Inhibitor in Multiple Sclerosis.. N Engl J Med, 380 (25):(2406-2417). [PMID:31075187]
3.Caldwell RD, Qiu H, Askew BC, Bender AT, Brugger N, Camps M, Dhanabal M, Dutt V, Eichhorn T, Gardberg AS et al.. (2019) Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases.. J Med Chem, 62 (17):(7643-7655). [PMID:31368705]
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B23011002