MSC2360844

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MSC2360844 是一种有效的、口服活性的、选择性的 PI3Kδ 抑制剂（IC50 为 145 nM）。

MSC2360844 is a potent, orally active and selective inhibitor of PI3Kδ(IC50 of 145 nM).(In Vitro):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.(In Vivo):in a murine SLE model，MSC2360844 ameliorates disease manifestations.

Roginolisib (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. Roginolisib inhibits B cell proliferation in a concentration-dependent manner with an IC50 of 48 nM. Roginolisib blocks BCR- and TCR-mediated responses in lymphocytes and TLR-induced IFNα by pDC in human primary cells. Cell Proliferation Assay Cell Line:B cells Concentration:0-10 μM Incubation Time:1 hour Result:Inhibited B cell proliferation in a concentration-dependent manner with an IC50 of 48 nM.

Roginolisib (6.6-66 mg/kg; daily from week 2 to 10) ameliorates disease manifestations in a murine SLE model. Animal Model:NZB/W F1 female mice 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.

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PI3K/Akt/mTOR signaling

PI3K

Apoptosis

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1305267-37-1

526.58

C26H27FN4O5S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (189.90 mM)

Fc1cccc2-c3c(CS(=O)(=O)c12)c(nn3-c1ccc(CN2CCOCC2)cc1)C(=O)N1CCOCC1

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(-20℃)

With Ice Pack

≥ 2 years