MSC2360844是一种有效的，具有口服活性的，选择性的PI3Kδ抑制剂，IC50为145nM。MSC2360844对一组278种其他激酶显示出高度选择性。
MSC2360844 is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. MSC2360844 shows highly selective against a panel of 278 additional kinases[1].
MSC2360844 (0-10 μM; 1 hours) completely abolished BCR-induced pAkt in Ramos B cells in a concentration-dependent manner with IC50 values of 280 nM[1]. MSC2360844 inhibits B cell proliferation in a concentration-dependent manner with an IC50 of 48 nM. MSC2360844 blocks BCR- and TCR-mediated responses in lymphocytes and TLR-induced IFNα by pDC in human primary cells[1]. Cell Proliferation Assay[1] Cell Line: B cells
MSC2360844 (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]
[1]. Haselmayer P, et al. Characterization of Novel PI3Kδ Inhibitors as Potential Therapeutics for SLE and Lupus Nephritis in Pre-Clinical Studies. Front Immunol. 2014 May 22;5:233.
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