AS-252424 化学構造
分子量: 305.28

高品質保証

カスタマーフィードバック(2)

Quality Control & MSDS

製品説明

  • Compare PI3K Inhibitors
    PI3K製品生物活性の比較
  • 研究分野

製品の説明

生物活性

製品説明 AS-252424は、PI3Kγの新しくて、強力で、選択的な阻害剤で、IC50 が 33 nMです。
ターゲット PI3Kγ CK2 (casein kinase 2) PI3Kα
IC50 33 nM 20 nM 935 nM [1]
In vitro試験 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試験 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]
臨床試験
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

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: [1]

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: [1]

動物モデル Intraperitoneally injecting female C3H mice with thioglycollate (40 ml/kg) to induced a peritonitis mouse model
製剤 AS-252424 is dissolved in vehicle (0.5% carboxymethylcellulose/0.25% Tween-20) and adjusted the solution to 10 mL/kg of body weight.
投薬量 10 mg/kg
投与方法 Oral administration 15 minutes before injection of thioglycollate

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download AS-252424 SDF
分子量 305.28
化学式

C14H8FNO4S

CAS No. 900515-16-4
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 61 mg/mL (199.81 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 0.5% CMC/0.25% Tween 80 30 mg/mL
* <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.
化学名 (Z)-5-((5-(4-fluoro-2-hydroxyphenyl)furan-2-yl)methylene)thiazolidine-2,4-dione

カスタマーフィードバック (2)


Click to enlarge
Rating
Source Inflammation, 2014, 37(4), 1254-60. AS-252424 purchased from Selleck
Method Immunoblot analysis
Cell Lines BMMCs
Concentrations 0-2.5 uM
Incubation Time 1 h
Results Then, we examined whether AS252424 inhibits phosphorylation of cPLA 2 and MAPKs. Immunoblotting result indicated that KL-dependent expression of p-cPLA 2 was dramatically increased after 15-min stimulation but suppressed by AS252424.

Click to enlarge
Rating
Source Dr. Zhang of Tianjin Medical University. AS-252424 purchased from Selleck
Method Western blot
Cell Lines A549 cells
Concentrations 0-10 μM
Incubation Time 3 h
Results AS-252424 treatment resulted in a reduction of AKT phosphorylation.

文献中の引用 (7)

技術サポート&よくある質問(FAQ)

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)

他の質問がある場合は、お気軽くお問合せください。

* 必須

Related PI3K 阻害剤

  • PI-3065

    PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, >70-fold selectivity over other PI3K family members.

  • GNE-317

    GNE-317 is a potent, brain-penetrant PI3K inhibitor.

  • Pilaralisib (XL147)

    Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2.

  • LY2090314

    LY2090314 は GSK-3α と GSK-3βのために、強力なGSK-3阻害剤で、IC50 がそれぞれ1.5 nM と 0.9 nMです。

  • LY294002

    LY294002は、p110α、p110δとp110βのPI3K阻害剤で、IC50 がそれぞれ 0.5 μM、0.57 μM、0.97 μMです。

  • 3-Methyladenine (3-MA)

    3-Methyladenine (3-MA) は選択の自噬とリン酸イノシトール3キナーゼ(キナーゼ)阻害剤、Vps34 と PI3Kγ に作用する時、 IC50 がそれぞれ 25 nM と 60 nM になる。自動食物胞の形成を妨害すること。

  • BEZ235 (NVP-BEZ235, Dactolisib)

    BEZ235 (NVP-BEZ235, Dactolisib)は競争性的なPI3K、mTOR 阻害剤、 p110α, p110γ, p110δ と p110β を作用すると、 IC50 がぞれぞれ 4 nM, 5 nM, 7 nM と 75 nMになる.

  • Wortmannin

    ワートマニンはミオシン軽鎖キナーゼ(MLCK)のマルチターゲットの阻害剤、IC50がぞれぞれ0.17μMと3nMになる。自動食物胞の形成を妨害すること。

  • Pictilisib (GDC-0941)

    Pictilisib (GDC-0941)は、PI3Kα、PI3Kβ、PI3KδとPI3Kγの強力な阻害剤で、IC50 がそれぞれ 3 nM、 33 nM、 3 nM、75 nMです。

  • CAL-101 (Idelalisib, GS-1101)

    CAL-101 (Idelalisib, GS-1101)は、2.5nMのIC50によるp110δの選択的なPI3KクラスI阻害剤です。

最近チェックしたアイテム

Tags: AS-252424を買う | AS-252424供給者 | AS-252424を購入する | AS-252424費用 | AS-252424生産者 | オーダーAS-252424 | AS-252424代理店
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description
お問い合わせ