產(chǎn)品目錄

規(guī)格	5mg 10mg 25mg
CAS	1254036-77-5
別名	N/A
化學名	6-?(1H-?indol-?4-?yl)?-?4-?[5-?[[4-?(1-?methylethyl)?-?1-?piperazinyl]?methyl]?-?2-?oxazolyl]?-1H-?indazole, monohydrochloride
分子式	C26H28N6O HCl
分子量	477.0
溶解度	≤0.2mg/ml in ethanol;20mg/ml in DMSO;14mg/ml in dimethyl formamide
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

pKi : 9.9

GSK2269557 is an inhibitor of PI3Kδ.

Phosphoinositide 3-kinase delta (PI3Kδ), a lipid kinase belonging to the Class 1 PI3K family, catalyzes the phosphorylation of phosphatidylinositol-4,5-bisphosphate to produce the critical signalling molecule phosphatidylinositol-3,4,5-triphosphate and then triggers various downstream biological events that ultimately regulate cell proliferation, growth, differentiation, chemotaxis and survival.

In vitro: In the screening study, GSK2269557 met the original potency goal in the PBMC assay (pIC50 >9) and showed exquisite selectivity against the PI3K isoforms in a modified HTRF assay. Moreover, GSK2269557 could induce concentration-dependent increases in QT interval and Tpe at 0.3 and 1 μM and an increase in QRS at 1 μM, however, no treatment-related TdP arrhythmias were seen [1].

In vivo: In a disease relevant Brown Norway Rat acute OVA model of Th2 driven lung inflammation, GSK2269557 was found to be albe to protect against eosinophil recruitment with an ED50 of 67 μg/kg. The activity of GSK2269557 was also assessed using other endpoints, leukocyte recruitment to the lung (neutrophils, macrophages, CD4 and CD8 T-lymphocytes at 48 hours) and Th2 cytokines such as IL-13. It was found that GSK2269557 could reduce recruitment of all leukocyte subpopulations and IL-13 in the lungs in a dose-dependent manner [1].

Clinical trial: GSK2269557 was investigated in a double blind and placebo controlled trial in healthy males and smokers. It was found that GSK2269557 was well tolerated in healthy males. There was a low incidence of AE’s and the plasma PK was well defined confirming high levels of drug within the lung compared to plasma [2].

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原創(chuàng)作者：上海莼試生物技術有限公司

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