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  2. PI3K/Akt/mTOR
  3. PI3K
  4. AS-252424

AS-252424 是一種有效的選擇性 PI3Kγ 抑制劑，IC50 為 30±10 nM。

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AS-252424 Chemical Structure

AS-252424 Chemical Structure

CAS No. : 900515-16-4

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥847
In-stock
1 mg ￥350
In-stock
5 mg ￥770
In-stock
10 mg ￥1400
In-stock
50 mg   詢價  
100 mg   詢價  

* Please select Quantity before adding items.

    AS-252424 purchased from MCE. Usage Cited in: J Mol Med (Berl). 2018 Feb;96(2):119-133.  [Abstract]

    The regulation of PHP14 on Akt phosphorylation is possibly via PI3Kγ in LX-2 cells. Cells are serum starvation 24 h, then treated TGF-β1 (10 ng/mL) 2 h, then added LY294002 (5 μM) or AS252424 (10 μM) as indicated; after another 2 h incubation, Western blot is performed to assess the protein expression of p-Akt.

    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    AS-252424 is a potent and selective PI3Kγ inhibitor with an IC50 of 30±10 nM.

    IC50 & Target[1]

    PI3Kα

    935 nM (IC50)

    PI3Kγ

    30 nM (IC50)

    PI3Kδ

    20 μM (IC50)

    PI3Kβ

    20 μM (IC50)

    體外研究
    (In Vitro)

    AS-252424 also inhibits PI3Kα, PI3Kβ and PI3Kδ with IC50s of 935±150 nM, 20 μM and 20 μM, respectively. 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. In the human monocytic cell line THP-1, MCP-1 binding to the GPCR chemokine receptor CCR2, strongly induces phosphorylation of PKB/Akt, which is effectively inhibited by AS-252424 at IC50 values as low as 0.4 μM. In contrast, induction of PKB/Akt phosphorylation by colony stimulating factor (CSF-1), binding to the growth factor receptor c-fms, is only blocked by AS-252424 at IC50 values as high as 4.7 μM[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    Oral administration of AS-252424 in a mouse model of acute peritonitis leads to a significant reduction of leukocyte recruitment. To evaluate the efficacy of AS-252424 to block leukocyte migration in vivo, it is tested in a mouse model of thioglycollate-induced peritonitis. Oral administration of AS-252424 at 10 mg/kg results in moderate reduction of neutrophil recruitment (35%±14%), almost matching the result observed in PI3Kγ-deficient mice. Given the short oral half-life of AS-252424 (t1/2=1 h) and relative high clearance (2.25 L/kg per h), investigations at later time points (24-48 h) to assess macrophage and monoycyte recruitment are not undertaken. The modest pharmacokinetic properties do not appear to be caused by rapid oxidative metabolism (microsomal metabolism after 1 h: 16% (rat), 10% (human))[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    305.28

    Formula

    C14H8FNO4S
    CAS 號
    性狀

    固體

    顏色

    Light yellow to brown

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : 25 mg/mL (81.89 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 3.2757 mL 16.3784 mL 32.7568 mL
    5 mM 0.6551 mL 3.2757 mL 6.5514 mL
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請?jiān)?年內(nèi)使用， -20°C儲存時，請?jiān)?年內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物溶解方案計算器
    請輸入動物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實(shí)驗(yàn)過程有損耗，建議您多配一只動物的量
    計算結(jié)果
    工作液所需濃度 : mg/mL
    純度 & 產(chǎn)品資料

    純度: 99.71%

    參考文獻(xiàn)
    Kinase Assay
    [1]

    A PI3Kγ lipid kinase assay, based on the neomycin-coated scintillation proximity assay (SPA) bead technology, is performed in 384-well plates using ATP/[γ33P]ATP and PtdIns. Kinase assays for IC50 value determinations with PI3Kα, PI3Kβ, and PI3Kδ are carried out[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [1]

    After 3 h of starvation in serum-free medium, Raw-264 macrophages are pretreated with inhibitors (e.g., AS-252424, 1 nM, 10 nM, 100 nM, 1 μM, 10 μM and 100 μM) or DMSO for 30 min and stimulated for 5 min with 50 nM C5a. PKB/Akt phosphorylation is monitored using phospho-Ser-473 Akt specific antibody and standard ELISA protocols[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice[1]
    PI3Kγ knockout (KO) mice are used. Oral administration of AS-252424 at 10 mg/kg is performed in PI3Kγ-deficient mice.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    參考文獻(xiàn)

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請?jiān)?年內(nèi)使用， -20°C儲存時，請?jiān)?年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.2757 mL 16.3784 mL 32.7568 mL 81.8920 mL
    5 mM 0.6551 mL 3.2757 mL 6.5514 mL 16.3784 mL
    10 mM 0.3276 mL 1.6378 mL 3.2757 mL 8.1892 mL
    15 mM 0.2184 mL 1.0919 mL 2.1838 mL 5.4595 mL
    20 mM 0.1638 mL 0.8189 mL 1.6378 mL 4.0946 mL
    25 mM 0.1310 mL 0.6551 mL 1.3103 mL 3.2757 mL
    30 mM 0.1092 mL 0.5459 mL 1.0919 mL 2.7297 mL
    40 mM 0.0819 mL 0.4095 mL 0.8189 mL 2.0473 mL
    50 mM 0.0655 mL 0.3276 mL 0.6551 mL 1.6378 mL
    60 mM 0.0546 mL 0.2730 mL 0.5459 mL 1.3649 mL
    80 mM 0.0409 mL 0.2047 mL 0.4095 mL 1.0237 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Inquiry Information

    產(chǎn)品名稱：
    AS-252424
    目錄號：
    HY-13532
    需求量：