MSC2360844 hemifumarate is a highly potent and orally active compound that acts as a selective inhibitor of PI3Kδ, with an IC50 value of 145 nM. This compound exhibits exceptional selectivity against a comprehensive panel of 278 additional kinases.

PI3Kδ:145 nM (IC50)

MSC2360844 hemifumarate (0-10 μM; 1 hours) completely abolished BCR-induced pAkt in Ramos B cells in a concentration-dependent manner with IC 50 values of 280?nM[1]. MSC2360844 hemifumarate inhibits B cell proliferation in a concentration-dependent manner with an IC 50 of 48?nM. MSC2360844 hemifumarate blocks BCR- and TCR-mediated responses in lymphocytes and TLR-induced IFNα by pDC in human primary cells[1]. Cell Viability Assay[1]Cell Line: B cells Concentration: 0-10 μM Incubation Time: 1 hour Result: Inhibited B cell proliferation in a concentration-dependent manner with an IC 50 of 48 nM.

MSC2360844 hemifumarate (6.6-66 mg/kg; daily from week 2 to 10) ameliorates disease manifestations in a murine SLE model[1]. Animal Model: NZB/W F1 female mice[1]Dosage: 6.6, 22, or 66?mg/kg Administration: Oral; starting at week 2 post ADV-IFNα delivery, once daily at 10?weeks Result: Significantly reduced proteinuria incidence and severity in a dose-dependent manner.