Roginolisib

Roginolisib (MSC2360844; IOA-244) is a potent, orally active and selective PI3Kδ inhibitor, with an IC 50 of 145 nM. Roginolisib shows highly selective against a panel of 278 additional kinases In Vitro Roginolisib (0-10 μM; 1 hours) completely abolished BCR-induced pAkt in Ramos B cells in a concentration-dependent manner with IC 50 values of 280?nM. Roginolisib inhibits B cell proliferation in a concentration-dependent manner with an IC 50 of 48?nM. Roginolisib blocks BCR- and TCR-mediated responses in lymphocytes and TLR-induced IFNα by pDC in human primary cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: B cells Concentration: 0-10 μM Incubation Time: 1 hour Result: Inhibited B cell proliferation in a concentration-dependent manner with an IC 50 of 48 nM. In Vivo Roginolisib (6.6-66 mg/kg; daily from week 2 to 10) ameliorates disease manifestations in a murine SLE model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. IC50& Target:PI3Kδ 145 nM (IC 50 ) PI3Kα 18500 nM (IC 50 ) PI3Kβ 2850 nM (IC 50 )

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