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, at concentrations ranging from 0 to 10 μM and a treatment duration of 1 hour, effectively eliminated BCR-triggered pAkt activation in Ramos B cells, displaying a concentration-dependent effect with an IC50 of 280 nM[1]. This compound also suppresses B cell proliferation in a similar concentration-dependent fashion, achieving an IC50 of 48 nM. Further, MSC2360844 hemifumarate impedes both BCR- and TCR-mediated responses in lymphocytes and inhibits TLR-induced IFNα production in pDC within human primary cells[1]. A Cell Viability Assay[1] using B cells, with the same concentration and incubation time parameters, confirmed the compound's capability to inhibit B cell proliferation in a concentration-dependent manner, noted by 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.