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

AS-252424 是一种有效的选择性 PI3Kγ 抑制剂，IC50 为 30±10 nM。

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AS-252424 Chemical Structure

AS-252424 Chemical Structure

CAS No. : 900515-16-4

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规格 价格 是否有货 数量
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   询价  
100 mg   询价  

* Please select Quantity before adding items.

AS-252424 相关抗体

Top Publications Citing Use of Products

    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.

    查看 PI3K 亚型特异性产品:

    查看所有亚型
    PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    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)

    体外研究
    (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.

    AS-252424 相关抗体:
    体内研究
    (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 号
    性状

    固体

    颜色

    Light yellow to yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 25 mg/mL (81.89 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 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
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料
    参考文献
    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.
    参考文献

    AS-252424 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 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.

    Keywords:

    AS-252424900515-16-4AS252424AS 252424PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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    目录号：
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