| Identification | Back Directory | [Name]
5H-Pyrrolo[2,3-b]pyrazine-7-carboxaMide, N-[(1R)-1-
[(3-cyano-1-azetidinyl)carbonyl]-2,2-diMethylpropyl]-2-cyclopropyl- | [CAS]
1334673-53-8 | [Synonyms]
JAK-IN-1
N-[(2R)-1-(3-cyanoazetidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl]-2-cyclopropyl-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
5H-Pyrrolo[2,3-b]pyrazine-7-carboxaMide, N-[(1R)-1-
[(3-cyano-1-azetidinyl)carbonyl]-2,2-diMethylpropyl]-2-cyclopropyl- | [Molecular Formula]
C20H24N6O2 | [MDL Number]
MFCD28386228 | [MOL File]
1334673-53-8.mol | [Molecular Weight]
380.444 |
| Hazard Information | Back Directory | [Description]
JAK-IN-1 is a novel potent JAK1/2/3 inhibitor. | [Uses]
JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and 3.2 nM, respectively. JAK-IN-1 shows improved selectivity for JAK3 over JAK1. | [in vivo]
JAK-IN-1 is JAK3 selective in vivo, as judged by higher potency inhibiting JAK1/JAK3- vs JAK2- or JAK1/JAK2/TYK2-driven signaling in whole blood assays. JAK-IN-1 potently inhibits IL-2 stimulated plasma concentrations of JAK-IN-1 for each dose. JAK-IN-1 prevents IL-2-driven STAT5 phosphorylation in a dose- and concentration-dependent manner, with approximately 50% inhibition observed at the 10 mg/kg dose (plasma concentration ～480 nM)[1]. | [storage]
Store at -20°C | [References]
[1] Soth M, et al. 3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models. J Med Chem. 2013 Jan 10;56(1):345-56. DOI:10.1021/jm301646k |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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