GSK2292767 - CAS 1254036-66-2
Catalog number: 1254036-66-2
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C24H28N6O5S
Molecular Weight:
512.58
COA:
Inquire
Targets:
PI3K
Description:
GSK2292767 is a Phosphatidylinositol 3 kinase delta inhibitor applicated for the treatment of respiratory diseases including asthma and COPD in clinical trials. GSK2292767 is highly selective for PI3Kδ over the closely related isoforms and is really active in the animal model of Th2-driven lung inflammation.
Purity:
98%
Appearance:
Powder
Synonyms:
GSK2292767; GSK-2292767; GSK 2292767. N-[5-[4-[5-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]methyl]-1,3-oxazol-2-yl]-1H-indazol-6-yl]-2-methoxypyridin-3-yl]methanesulfonamide;SCHEMBL173490;ZINC95938263;KB-78330;1254036-66-2;Methanesulfonamide,N-[5-[4-[5-[[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-methoxy-3-pyridinyl]
Solubility:
Soluble in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
asthma and COPD
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
NLUPPCTVKHDVIQ-GASCZTMLSA-N
InChI:
InChI=1S/C24H28N6O5S/c1-14-11-30(12-15(2)34-14)13-18-9-26-23(35-18)19-5-16(6-21-20(19)10-27-28-21)17-7-22(29-36(4,31)32)24(33-3)25-8-17/h5-10,14-15,29H,11-13H2,1-4H3,(H,27,28)/t14-,15+
Canonical SMILES:
CC1CN(CC(O1)C)CC2=CN=C(O2)C3=C4C=NNC4=CC(=C3)C5=CC(=C(N=C5)OC)NS(=O)(=O)C
Current Developer:
GSK
1.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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CAS 1254036-66-2 GSK2292767

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