Roginolisib hemifumarate

• CAT Number: I045752
• CAS Number: 1621688-31-0
• Molecular Formula: C26H27FN4O5S.1/2C4H4O4
• Molecular Weight: 584.62
• Purity: ≥95%

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[1].
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[1].
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[1].
Roginolisib hemifumarate (6.6-66 mg/kg; daily from week 2 to 10) ameliorates disease manifestations in a murine SLE model[1].

Reference

[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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