MSC2360844hemifumarate是一种有效的，具有口服活性的选择性PI3Kδ抑制剂，IC50为145nM。MSC2360844hemifumarate对一组278种其他激酶显示出高度选择性。
货号:ajcx31124
CAS:1621688-31-0
分子式:C26H27FN4O5S.1/2C4H4O4
分子量：584.62
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

MSC2360844 hemifumarate is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. MSC2360844 hemifumarate shows highly selective against a panel of 278 additional kinases[1].

MSC2360844 hemifumarate (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 hemifumarate inhibits B cell proliferation in a concentration-dependent manner with an IC50 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

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]

[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.