AS-252424

製品コードS2671 バッチS267102

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

C14H8FNO4S
分子量 305.28 CAS No. 900515-16-4
Solubility (25°C)* 体外 DMSO 61 mg/mL (199.81 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
4%DMSO 50%PEG300 5%Tween80 41%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 40 μL of 125 mg/ml clarified DMSO stock solution to 500 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 410 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 AS-252424 is a novel, potent PI3Kγ inhibitor with IC50 of 30 nM in a cell-free assay with 30-fold selectivity for PI3Kγ than PI3Kα, and low inhibitory activity towards PI3Kδ/β.
in vitro AS-252424 is a furan-2-ylmethylene thiazolidinedione as a selective ATP-competitive PI3Kγ inhibitor with IC50 with 33 nM. AS-252424 shows reduced potency on PI3Kα with an IC50 with 935 nM. When screening against 80 different Ser/Thr and Tyr kinases, AS-252424 doesn't show significant inhibit towards any of them at 10 μM except for CK2. AS-252424 inhibits C5a-mediated PKB/Akt phosphorylation in a concentration- dependent manner with submicromolar or low-micromolar IC50 value. AS-252424 inhibits MCP-1-mediated chemotaxis in wild-type primary monocytes in a concentration-dependent manner with an IC50 value of 52 μM, as well as in the monocytic cell line THP-1 with an IC50 value of 53 μM. [1] AS252424 specifically blocks proliferation in the pancreatic cancer cell lines HPAF and Capan1, as assessed by cell counting. [2] A recent research indicates 100 nM of AS-252424 significantly reduces [Ca2+]i, ICa and Ca2+ transients in HL-1 cardiomyocytes. [3]
in vivo Oral administration of AS-252424 at 10 mg/kg results in moderate reduction of neutrophil recruitment (35%), almost matching the result observed in PI3Kγ-deficient mice. [1]

プロトコル(参考用のみ)

キナーゼアッセイ In vitro PI3Kγ Kinase Assay
Human PI3Kγ (100 ng) is incubated at RT with kinase buffer (10 mM MgCl2, 1 mM β-glycerophosphate, 1 mM DTT, 0.1 mM Na3VO4, 0.1% Na Cholate and 15 M ATP/100 nCi γ[33]ATP, final concentrations) and lipid vesicles containing 18 M PtdIns and 250 M of PtdSer (final concentrations), in the presence of AS-252424 or DMSO. Kinase reaction is stopped by adding 250 g of Neomycin-coated Scintillation Proximity Assay (SPA) beads and preceded.
細胞アッセイ 細胞株 Raw-264 macrophage
濃度 0.01 nM to 0.1 μM
反応時間 5 minutes
実験の流れ After 3 hours of starvation in serum-free medium, Raw-264 macrophages are pretreated with AS-252424 or DMSO for 30 minutes and stimulated for 5 minutes with 50 nM C5a. PKB/Akt phosphorylation is monitored using phospho-Ser-473 Akt specific antibody and standard ELISA protocols.
動物実験 動物モデル Intraperitoneally injecting female C3H mice with thioglycollate (40 ml/kg) to induced a peritonitis mouse model
投薬量 10 mg/kg
投与方法 Oral administration 15 minutes before injection of thioglycollate

カスタマーフィードバック

Data from [Data independently produced by Inflammation, 2014, 37(4), 1254-60]

, , Dr. Zhang of Tianjin Medical University

Data from [Data independently produced by , , Inflammation, 2017, 40(2):435-441]

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：

Upregulated Apelin Signaling in Pancreatic Cancer Activates Oncogenic Signaling Pathways to Promote Tumor Development [ Int J Mol Sci, 2022, 23-1810600] PubMed: 36142542
Distinct roles of PI3Kδ and PI3Kγ in a toluene diisocyanate-induced murine asthma model [ Toxicology, 2021, 454:152747] PubMed: 33711354
Soluble Epoxide Hydrolase Inhibitors Regulate Ischemic Arrhythmia by Targeting MicroRNA-1 [ Front Physiol, 2021, 12:717119] PubMed: 34646152
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
Frailty is associated with neutrophil dysfunction which is correctable with phosphoinositol-3-kinase inhibitors [ J Gerontol A Biol Sci Med Sci, 2020, glaa216] PubMed: 32877922
Targeting effector pathways in RAC1P29S-driven malignant melanoma. [ Small GTPases, 2020, 10.1080/21541248] PubMed: 32043900
Myocyte enhancer factor 2A delays vascular endothelial cell senescence by activating the PI3K/p-Akt/SIRT1 pathway [ Aging (Albany NY), 2019, 11(11):3768-3784] PubMed: 31182679
Critical roles for the phosphatidylinositide 3-kinase isoforms p110β and p110γ in thrombopoietin-mediated priming of platelet function [ Sci Rep, 2019, 9(1):1468] PubMed: 30728366
Role of PI3K/Akt and MEK/ERK Signalling in cAMP/Epac-Mediated Endothelial Barrier Stabilisation. [ Front Physiol, 2019, 10:1387] PubMed: 31787905
PI3Ka-Akt1-mediated Prdm4 induction in adipose tissue increases energy expenditure, inhibits weight gain, and improves insulin resistance in diet-induced obese mice [ Cell Death Dis, 2018, 9(9):876] PubMed: 30158592

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。