GSK-2292767 ( GSK2292767 | GSK-2292767 | GSK 2292767 )

产品货号. M11026 CAS No. 1254036-66-2

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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产品名称

GSK-2292767
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

GSK-2269557 是一种高效、选择性的 PI3Kδ 抑制剂 (pKi=10.1)。
产品描述

GSK-2269557 is a highly potent and selective inhibitor of PI3Kδ (pKi=10.1); displays >1,000 fold selectivity versus others PI3K isoforms; inhibits both IFNγ and IL-2 production in a concentration-dependent manner, with pIC50 values of 8.7 and 8.5, respectively, in a human lung parenchyma assay; shows activity in rat acute OVA model of Th2-driven lung inflammation (ED50=35 ug/kg).COPD Phase 1 Clinical.
体外实验

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体内实验

GSK2292767 exhibits high clearance (50 mL/min/kg) in vivo and low oral bioavailability (F < 2%) in a rat PK study.GSK2292767 (0.01-1 μM) has no e?ect on QT interval, Tp?e, or QRS and no signi?cant risk of TdP arrhythmias in a rabbit cardiac ventricular wedge assay.GSK2292767 protects against eosinophil recruitment with an ED50 of 35 μg/kg in the brown Norway rat acute OVA model of Th2 driven in?ammation in the lungs of rats.
同义词

GSK2292767 | GSK-2292767 | GSK 2292767
通路

PI3K/Akt/mTOR signaling
靶点

PI3K
受体

PI3Kδ
研究领域

Inflammation/Immunology
适应症

COPD

CAS Number

1254036-66-2
分子量

512.58
分子式

C24H28N6O5S
纯度

>98% (HPLC)
溶解度

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SMILES

CS(=O)(NC1=CC(C2=CC3=C(C(C4=NC=C(CN5C[C@@H](C)O[C@@H](C)C5)O4)=C2)C=NN3)=CN=C1OC)=O
化学全称

N-(5-(4-(5-(((2R,6S)-2,6-dimethylmorpholino)methyl)oxazol-2-yl)-1H-indazol-6-yl)-2-methoxypyridin-3-yl)methanesulfonamide