| Identification | Back Directory | [Name]
MSC2360844 hemifumarate | [CAS]
1621688-31-0 | [Synonyms]
MSC2360844 hemifumarate Roginolisib (IOA-244) hemifumarate | [Molecular Formula]
C30H31FN4O9S | [MOL File]
1621688-31-0.mol | [Molecular Weight]
642.66 |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
Roginolisib 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] | | 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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| [IC 50]
PI3Kδ: 145 nM (IC50) | [References]
[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. DOI:10.3389/fimmu.2014.00233 |
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