ChemicalBook--->CAS DataBase List--->1621688-31-0

1621688-31-0

1621688-31-0 Structure

1621688-31-0 Structure
IdentificationBack 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
Chemical PropertiesBack Directory
[form ]

Solid
[color ]

White to off-white
Hazard InformationBack 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.
[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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