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HS-173

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Chemical Structure| 1276110-06-5 同义名 : -
CAS号 : 1276110-06-5
货号 : A336342
分子式 : C21H18N4O4S
纯度 : 99%+
分子量 : 422.457
MDL号 : MFCD28023584
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(118.36 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+30% PEG300+water 4 mg/mL clear

PO 0.5% CMC-Na 34 mg/mL suspension

生物活性
靶点

  • p110α

    PI3Kα , IC50:0.8 nM
描述 HS-173, at concentrations ranging from 0.1 to 10 μM, diminishes cell viability in a manner that is both concentration and time-dependent. It effectively curbs the growth of colonies in pancreatic cancer cells as the dosage increases. Moreover, HS-173 blocks cell migration and invasion triggered by TGF-β in pancreatic cancer cells and prevents TGF-β-induced epithelial-mesenchymal transition (EMT)[1]. In experiments with two hepatic stellate cell lines, HS-173 application leads to a reduction in cell viability, influenced by the dosage and duration of treatment. It prompts a halt in the cell cycle at the G2/M phase. The compound elevates levels of cleaved caspase-3 and reduces those of Bcl-2 in HSC-T6 cells. Furthermore, HS-173 curtails the expression of pro-fibrotic mediators and modulators of extracellular matrix (ECM) degradation in hepatic stellate cells (HSCs)[2]. The co-administration of Sorafenib and HS-173 acts synergistically to halt cell proliferation in pancreatic cancer cell lines, affecting crucial enzymes within the RAF/MAPK and PI3K/AKT signaling pathways[3].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
MCF7 cells Cytotoxicity assay 48 h Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50=7.8 μM 21388141
SK-BR-3 cells Cytotoxicity assay 48 h Cytotoxicity against human SK-BR-3 cells after 48 hrs by MTT assay, IC50=1.5 μM 21388141
T47D cells Cytotoxicity assay 48 h Cytotoxicity against human T47D cells after 48 hrs by MTT assay, IC50=0.6 μM 21388141
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.37mL

0.47mL

0.24mL

11.84mL

2.37mL

1.18mL

23.67mL

4.73mL

2.37mL
参考文献

[1]Rumman M, et al. HS-173, a novel PI3K inhibitor suppresses EMT and metastasis in pancreatic cancer. Oncotarget. 2016 Oct 25

[2]Son MK, et al. HS-173, a novel PI3K inhibitor, attenuates the activation of hepatic stellate cells in liver fibrosis. Sci Rep. 2013 Dec 11;3:3470

[3]Yun SM, et al. Synergistic anticancer activity of HS-173, a novel PI3K inhibitor in combination with Sorafenib against pancreatic cancer cells. Cancer Lett. 2013 May 1;331(2):250-61