GSK2269557 - CAS 1254036-71-9
Catalog number: 1254036-71-9
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
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GSK2269557, an effective PI3K inhibitor, could be used as against inflammatory and some autoimmune diseases. It has just completes a phase II trial against Asthma.
CHEMBL2216859; GSK2269557 (free base); GSK2269557; GSK-2269557; GSK 2269557; Nemiralisib; 2-(6-(1H-indol-4-yl)-1H-indazol-4-yl)-5-((4-isopropylpiperazin-1-yl)methyl)oxazole; 6-(1H-indol-4-yl)-4-(5-{[4-(1-methylethyl)-1-piperazinyl]methyl}-1,3-oxazol-2-yl)-1H-indazole
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GSK2269557 is an effective PI3K inhibitor that could be used as against inflammatory and some autoimmune diseases.
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
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1.Safety, Tolerability, and Pharmacokinetics of Single and Repeat Doses of Nemiralisib Administered via the Ellipta Dry Powder Inhaler to Healthy Subjects.
Wilson R;Jarvis E;Montembault M;Hamblin JN;Hessel EM;Cahn A Clin Ther. 2018 Aug;40(8):1410-1417. doi: 10.1016/j.clinthera.2018.06.011. Epub 2018 Jul 25.
PURPOSE: ;Novel therapies to treat chronic obstructive pulmonary disease are highly desirable. The safety, tolerability, and pharmacokinetic (PK) parameters of nemiralisib, a phosphoinositide 3-kinase δ inhibitor, administered via the Ellipta dry powder inhaler (GlaxoSmithKline, Research Triangle Park, North Carolina) was evaluated, including an assessment of oral bioavailability.;METHODS: ;This single-center, 3-part, placebo-controlled trial in 22 healthy subjects evaluated single (100 and 200 μg) and repeat (200 μg for 10 days) doses of inhaled nemiralisib in parts A (n = 12) and B (n = 12) (double-blind) and single doses of inhaled nemiralisib (200 µg) with and without charcoal block in Part C (n = 6) (open-label, 2-period, crossover). There was a minimum 14-day washout period between dosing days.;FINDINGS: ;21 subjects completed the study, mean age was similar in the three parts (A: 49 years; B: 44 years; C: 55 years). After single doses of nemiralisib, observed plasma C;max; dropped rapidly, followed by a slower elimination phase. Near-dose proportionality was observed: mean (95% CI) plasma C;max; and AUC;0-24; values were 174.3 pg/mL (96.9-313.3) and 694.6 pg·h/mL (503.5-958.2) for 100 μg and 398.
2.Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease.
Down K;Amour A;Baldwin IR;Cooper AW;Deakin AM;Felton LM;Guntrip SB;Hardy C;Harrison ZA;Jones KL;Jones P;Keeling SE;Le J;Livia S;Lucas F;Lunniss CJ;Parr NJ;Robinson E;Rowland P;Smith S;Thomas DA;Vitulli G;Washio Y;Hamblin JN J Med Chem. 2015 Sep 24;58(18):7381-99. doi: 10.1021/acs.jmedchem.5b00767. Epub 2015 Sep 3.
Optimization of lead compound 1, through extensive use of structure-based design and a focus on PI3Kδ potency, isoform selectivity, and inhaled PK properties, led to the discovery of clinical candidates 2 (GSK2269557) and 3 (GSK2292767) for the treatment of respiratory indications via inhalation. Compounds 2 and 3 are both highly selective for PI3Kδ over the closely related isoforms and are active in a disease relevant brown Norway rat acute OVA model of Th2-driven lung inflammation.
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