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MethanesulfonaMide, N-[5-[4-[5-[[(2R,6S)-2,6-diMethyl-4-Morpholinyl]Methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-Methoxy-3-pyridinyl]-, rel-

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MethanesulfonaMide, N-[5-[4-[5-[[(2R,6S)-2,6-diMethyl-4-Morpholinyl]Methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-Methoxy-3-pyridinyl]-, rel- Suppliers list
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MethanesulfonaMide, N-[5-[4-[5-[[(2R,6S)-2,6-diMethyl-4-Morpholinyl]Methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-Methoxy-3-pyridinyl]-, rel- manufacturers
MethanesulfonaMide, N-[5-[4-[5-[[(2R,6S)-2,6-diMethyl-4-Morpholinyl]Methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-Methoxy-3-pyridinyl]-, rel- Basic information
Product Name:MethanesulfonaMide, N-[5-[4-[5-[[(2R,6S)-2,6-diMethyl-4-Morpholinyl]Methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-Methoxy-3-pyridinyl]-, rel-
Synonyms:N-{5-[4-(5-{[(2R,6S)-2,6-Dimethyl-4-morpholinyl]methyl}-1,3-oxazo l-2-yl)-1H-indazol-6-yl]-2-methoxy-3-pyridinyl}methanesulfonamide;N-[5-[4-(5-{[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-oxazol-2-yl)-1H-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methanesulfonamide;CS-2341;PI3Kδ inhibitor GS2292767;MethanesulfonaMide, N-[5-[4-[5-[[(2R,6S)-2,6-diMethyl-4-Morpholinyl]Methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-Methoxy-3-pyridinyl]-, rel-;GSK2292767;rel-N-[5-[4-[5-[[(2R,6S)-2,6-Dimethyl-4-morpholinyl]methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-methoxy-3-pyridinyl]methanesulfonamide
CAS:1254036-66-2
MF:C24H28N6O5S
MW:512.58
EINECS:
Product Categories:
Mol File:1254036-66-2.mol
MethanesulfonaMide, N-[5-[4-[5-[[(2R,6S)-2,6-diMethyl-4-Morpholinyl]Methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-Methoxy-3-pyridinyl]-, rel- Structure
MethanesulfonaMide, N-[5-[4-[5-[[(2R,6S)-2,6-diMethyl-4-Morpholinyl]Methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-Methoxy-3-pyridinyl]-, rel- Chemical Properties
Melting point 199-202°C
Boiling point 730.4±70.0 °C(Predicted)
density 1.360±0.06 g/cm3(Predicted)
storage temp. -20°C Freezer, Under inert atmosphere
solubility DMSO (Slightly), Methanol (Slightly)
form Solid
pka6.29±0.50(Predicted)
color White to Off-White
Safety Information
MSDS Information
MethanesulfonaMide, N-[5-[4-[5-[[(2R,6S)-2,6-diMethyl-4-Morpholinyl]Methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-Methoxy-3-pyridinyl]-, rel- Usage And Synthesis
Usesrel-N-[5-[4-[5-[[(2R,6S)-2,6-Dimethyl-4-morpholinyl]methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-methoxy-3-pyridinyl]methanesulfonamide is a selective PI3Kδ inhibitor for the treatment of respiratory disease (1,2).
Biological Activitypki: 10.1gsk2292767 is a potent and selective pi3kδ inhibitor.phosphoinositide 3-kinase δ (pi3kδ), a lipid kinase belonging to the class 1 pi3k family with the closely homologous isoforms α and β, catalyzes the phosphorylation of phosphatidylinositol 4,5-bisphosphate, triggering various downstream biological events suvch as cell growth, proliferation, differentiation, and survival.
in vitrogsk2292767 was found to be greater than 100-fold selective against a panel of in-house kinases and in the millipore panel. moreover, gsk2292767 could inhibit both ifnγ and il-2 production in a concentration-dependent manner in a human lung parenchyma assay, with pic50s of 8.7 and 8.5, respectively [1].
in vivoin a rat pk study, the in vivo clearance for gsk2292767 was significantly higher than that for its analog gsk2269557. the oral bioavailability was also low (f < 2%), which was consistent with the data observed for gsk2269557. in a rabbit cardiac ventricular wedge assay, no effect on qt interval, tpe, or qrs and no significant risk of tdp arrhythmias was observed for gsk2292767 over the concentration range tested, thus indicating gsk2292767 could successfully mitigate the risk associated with gsk2269557. moreover, gsk2292767 was found to protect against eosinophil recruitment with an ed50 of 35 μg/kg in the brown norway rat acute ova model, which was similar to gsk2269557 [1].
IC 50PI3Kδ: 10.1 (pIC50)
references[1] down k et al. optimization of novel indazoles as highly potent and selective inhibitors of phosphoinositide 3-kinase δ for the treatment of respiratory disease. j med chem. 2015 sep 24;58(18):7381-99.
MethanesulfonaMide, N-[5-[4-[5-[[(2R,6S)-2,6-diMethyl-4-Morpholinyl]Methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-Methoxy-3-pyridinyl]-, rel- Preparation Products And Raw materials
Tag:MethanesulfonaMide, N-[5-[4-[5-[[(2R,6S)-2,6-diMethyl-4-Morpholinyl]Methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-Methoxy-3-pyridinyl]-, rel-(1254036-66-2) Related Product Information
GSK2126458 1-[(3,4-dichlorophenyl)methyl]-N-[4-(hydroxymethyl)phenyl]-5-methyl-1H-1,2,3-triazole-4-carboxamide GSK-2256098 GSK369796 GSK2982772 GSK2636771 GSK-2881078 gsk2200150a GSK-2018682 GSK 2239633A Lp-PLA2 -IN-1 GSK-3326595