| Identification | Back Directory | [Name]
MSC2360844 | [CAS]
1305267-37-1 | [Synonyms]
MSC2360844
MSC2360844(IOA-244 /roginolisib)
(6-fluoro-1-(4-(morpholinomethyl)phenyl)-5,5-dioxido-1,4-dihydrothiochromeno[4,3-c]pyrazol-3-yl)(morpholino)methanone
Phosphoinositide 3-kinase,MSC 2360844,MSC2360844,cells,SLE-prone,primary,Inhibitor,functions,inhibit,PI3K,proliferation,MSC-2360844
Methanone, [6-fluoro-1,4-dihydro-1-[4-(4-morpholinylmethyl)phenyl]-5,5-dioxido[1]benzothiopyrano[4,3-c]pyrazol-3-yl]-4-morpholinyl- | [Molecular Formula]
C26H27FN4O5S | [MDL Number]
MFCD32858274 | [MOL File]
1305267-37-1.mol | [Molecular Weight]
526.58 |
| Chemical Properties | Back Directory | [Boiling point ]
779.8±60.0 °C(Predicted) | [density ]
1.50±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
6.05±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Roginolisib (MSC2360844; IOA-244) is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. Roginolisib shows highly selective against a panel of 278 additional kinases[1]. | [in vivo]
Roginolisib (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); PI3Kα: 18500 nM (IC50); PI3Kβ: 2850 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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