13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
在線訂購 免費訂購熱線：021-59541103 021-60443211
標簽:GSK2269557
聯系人:高小姐
電話:021-59541103 021-60443211
手機:13585831301
Q Q： 3004967995
Email:3004967995@qq.com
詳細地址：上海嘉定區嘉羅公路1661
化學性質：
| 規格 | 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 |
產品描述：
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].
特別提醒：
1. 本產品僅供科研使用。請勿用于醫藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區。
2. 為了您的安全和健康，請穿好實驗服并佩戴一次性手套和口罩操作。
原創作者：上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名：上海生物
開 戶 行：中國銀行山東省分行營業部
賬 號：2169 2341 6278
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