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SF1670

现货
Catalog No.
B4787
PTEN抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 600.00
现货
10mg
¥ 950.00
现货
50mg
¥ 3,990.00
Ship with 10-15 days

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Background

SF1670 is a potent and specific inhibitor of PTEN [1].

Phosphatase and tensin homolog deleted on chromosome 10 (PTEN) is a phosphatidylinositol 3’-phosphatase that converts PtdIns(3,4,5)P3 to phosphatidylinositol 4,5-bisphosphate. PTEN functions as a tumor suppressor that is mutated in many cancers [1].

SF1670 is a potent and specific PTEN inhibitor. SF1670 bound to the active site of PTEN and increased PtdIns(3,4,5)P3 signaling in neutrophils. In human neutrophils, SF1670 significantly increased Akt phosphorylation stimulated by chemoattractant and specifically increased PtdIns(3,4,5)P3 signaling. SF1670 efficiently increased Akt phosphorylation at the concentration of 250nM. In mouse neutrophils, SF1670 also increased Akt phosphorylation and PtdIns(3,4,5)P3 signaling, which was mediated by the inhibition of PTEN activity. In neutrophils, SF1670 significantly increased reactive oxygen species (ROS) production induced by fMLP. Also, SF1670 increased neutrophil polarization induced by fMLP, which was necessary for the chemotactic migration and neutrophil recruitment to sites of inflammation [1].

In a mouse neutropenia-associated bacterial pneumonia model, SF1670 increased the bacteria-killing capability and relieved inflammation-associated lung damage [1].

Reference:
[1].  Li Y, Prasad A, Jia Y, et al. Pretreatment with phosphatase and tensin homolog deleted on chromosome 10 (PTEN) inhibitor SF1670 augments the efficacy of granulocyte transfusion in a clinically relevant mouse model. Blood, 2011, 117(24): 6702-6713.

Chemical Properties

Physical AppearanceA solid
StorageDesiccate at -20°C
M.Wt307.34
Cas No.345630-40-2
FormulaC19H17NO3
Solubility≥15.37mg/mL in DMSO
Chemical NameN-(9,10-dioxo-9,10-dihydrophenanthren-2-yl)pivalamide
SDFDownload SDF
Canonical SMILESCC(C)(C(NC(C=C1C2=O)=CC=C1C3=C(C2=O)C=CC=C3)=O)C
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

移植的小鼠嗜中性粒细胞

溶解方法

该化合物在DMSO中的溶解度大于15.4 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

500 nM

应用

在移植的嗜中性粒细胞中,SF1670增强PtdIns(3,4,5)P3信号。在鼠细胞中,SF1670升高Akt磷酸化。SF1670的预处理显著增加小鼠嗜中性粒细胞中的PtdIns(3,4,5)P3水平。在500 nM fMLP刺激的嗜中性粒细胞中,SF1670(500 nM)预处理引起较高的的超氧化物生成。

动物实验[1]:

动物模型

中性粒细胞小鼠

给药剂量

静脉注射,500 nM

应用

在腹膜炎和细菌性肺炎的中性粒细胞小鼠中,静脉注射500 nM剂量的SF1670增强了细菌杀伤能力,降低了中性粒细胞减少相关性肺炎的死亡率。 在小鼠中性粒细胞减少相关细菌性肺炎模型中,SF1670增加了细菌杀伤能力,减轻了炎症相关的肺损伤。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Li Y, Prasad A, Jia Y, et al. Pretreatment with phosphatase and tensin homolog deleted on chromosome 10 (PTEN) inhibitor SF1670 augments the efficacy of granulocyte transfusion in a clinically relevant mouse model[J]. Blood, 2011, 117(24): 6702-6713.

质量控制

化学结构

SF1670