HS-173

製品コードS7356 バッチS735602

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C21H18N4O4S
分子量 422.46 CAS No. 1276110-06-5
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 42 mg/mL (99.41 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 30%PEG300 5%Tween80 60%ddH2O
8.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 160 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 600 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM.
in vitro HS-173 shows potent antiproliferative effects in T47D, SK-BR3, and MCF7 cells with IC50 of 0.6, 1.5, and 7.8 μM, respectively. [1] HS-173 causes complete suppression of the PI3K pathway in cancer cell lines (Hep3B and SkBr3). Moreover, HS-173 induces cell apoptosis by affecting cell-cycle distribution and activating caspases, and block VEGF-induced angiogenesis in vitro. [2] Combined treatment with Sorafenib and HS-173 has a synergistic anti-cancer effect on pancreatic cancer cells. [3]
in vivo HS-173 diminishes blood vessel formation in mice. [2] HS-173 markedly attenuates the development of liver fibrosis by blocking PI3K/Akt signaling in vivo. [4]
特徴 PI3Kα-selective inhibitor.

プロトコル(参考用のみ)

キナーゼアッセイ PI3-Kinase assay
The PI3K assay is performed using the Kinase-Glo Max luminescent kinase assay kit which quantifies the amount of ADP produced by the PI3K reaction. In brief, an active PI3K (100 ng) is preincubated with compound for 5 min in kinase reaction buffer (25 mM MOPS [pH 7.0], 5 mM MgCl2, and 1 mM EGTA) and 10 μg l-α-phosphatidylinositol (PI). Before addition of PI, it is sonicated with sonication buffer (25 mM MOPS [pH 7.0], 1 mM EGTA) in water for 20 min for allowing miscelle formation. Then reaction is started by the addition of 10 μM ATP and ran for 180 min. To terminate kinase reaction, same volume of Kinase-Glo Max buffer is added. After 10 min, the plates are then read on a GloMax plate reader for luminescence detection.
細胞アッセイ 細胞株 T47D, SK-BR3, MCF7 cells
濃度 ~50 μM
反応時間 48 hours
実験の流れ Cell viability is performed by a MTT assay. Briefly, T47D cells are plated in 96-well plates for 24 h. Then, the medium is removed and cells were treated with either DMSO as a control or various concentrations of inhibitors. The final concentration of DMSO in the medium was ≤0.1% (v/v). After the cells are incubated for 48 h, 20 μL MTT solution (5 mg/mL) is added to each well for another 4 h at 37 °C. The formazan crystals that formed are dissolved in DMSO (100 μL/well) by constant shaking for 5 min. The plate is then read on a microplate reader at 540 nm. Three replicate wells are used for each analysis. The median inhibitory concentration (IC50, defined as the drug concentration at which cell growth is inhibited by 50%) is assessed from the dose−response curves. To assess the effect of compounds on cell proliferation, T47D cells are cultured with compound (0.1−100 μM) for 48 h before MTT analysis.
動物実験 動物モデル Male BALB/c mice with CCl4-induced liver fibrosis
投薬量 ~20 mg/kg
投与方法 p.o.

カスタマーフィードバック

, , Cancer Cell Int, 2017, 17:27

Data from [Data independently produced by , , Otorhinolaryngol Head Neck Surg, 2016, 1(2): 44-50.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Lipophagy-related gene RAB7A is involved in immune regulation and malignant progression in hepatocellular carcinoma [ Comput Biol Med, 2023, 158:106862] PubMed: 37044053
ABCB1 and ABCG2 Overexpression Mediates Resistance to the Phosphatidylinositol 3-Kinase Inhibitor HS-173 in Cancer Cell Lines [ Cells, 2023, 12(7)1056] PubMed: 37048130
The Pro-Fibrotic Response to Lens Injury Is Signaled in a PI3K Isoform-Specific Manner [ Biomolecules, 2022, 12-91181] PubMed: 36139020
Advancement of PI3 Kinase Inhibitor Combination Therapies for PI3K-Aberrant Chordoma [ J Neurol Surg B Skull Base, 2022, 83(1):87-98] PubMed: 35155075
The inhibitors of KDM4 and KDM6 histone lysine demethylases enhance the anti-growth effects of erlotinib and HS-173 in head and neck cancer cells [ Eur J Pharm Sci, 2021, 166:105961] PubMed: 34363938
Soluble Epoxide Hydrolase Inhibitors Regulate Ischemic Arrhythmia by Targeting MicroRNA-1 [ Front Physiol, 2021, 12:717119] PubMed: 34646152
Topical Application of the PI3Kβ-Selective Small Molecule Inhibitor TGX-221 Is an Effective Treatment Option for Experimental Epidermolysis Bullosa Acquisita [ Front Med (Lausanne), 2021, 8:713312] PubMed: 34557502
Topical Application of the PI3Kβ-Selective Small Molecule Inhibitor TGX-221 Is an Effective Treatment Option for Experimental Epidermolysis Bullosa Acquisita [ Front Med (Lausanne), 2021, 8:713312] PubMed: 34557502
Idelalisib Rescues Natural Killer Cells from Monocyte-Induced Immunosuppression by Inhibiting NOX2-Derived Reactive Oxygen Species [ Cancer Immunol Res, 2020, 8(12):1532-1541] PubMed: 32967913
Low dose novel PARP-PI3K inhibition via nanoformulation improves colorectal cancer immunoradiotherapy [ Mater Today Bio, 2020, 8:100082] PubMed: 33294836

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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