产品
编 号:F622534
分子式:C26H27FN4O5S.1/2C4H4O4
分子量:584.62
产品类型
结构图
CAS No: 1621688-31-0
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产品详情
生物活性:
Roginolisib (MSC2360844) hemifumarate is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. Roginolisib hemifumarate shows highly selective against a panel of 278 additional kinases.
体内研究:
Roginolisib hemifumarate (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.
体外研究:
Roginolisib 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. Roginolisib hemifumarate inhibits B cell proliferation in a concentration-dependent manner with an IC50 of 48 nM. Roginolisib hemifumarate blocks BCR- and TCR-mediated responses in lymphocytes and TLR-induced IFNα by pDC in human primary cells.