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  2. PI3K/Akt/mTOR Autophagy
  3. PI3K Autophagy
  4. ZSTK474

ZSTK474 是一種 ATP 競爭性的泛 I 類 PI3K 抑制劑，抑制 PI3Kα，PI3Kβ，PI3Kδ 和 PI3Kγ，IC50 分別為 16 nM，44 nM，4.6 nM 和 49 nM。

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ZSTK474 Chemical Structure

ZSTK474 Chemical Structure

CAS No. : 475110-96-4

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥338
In-stock
5 mg ￥308
In-stock
10 mg ￥515
In-stock
50 mg ￥1700
In-stock
100 mg ￥3100
In-stock
200 mg ￥4863
In-stock
500 mg   詢價  
1 g   詢價  

* Please select Quantity before adding items.

Customer Review

    ZSTK474 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Jun 25;37(1):122.  [Abstract]

    MHCC97H cells are treated with either LY294002 (2.5, 5,10, 20, 40 μM) or ZSTK474 (0.5, 1, 2.5, 5, 10 μM) for 24 h. DMSO is used as the control. Cell lysates are subjected to western blot analysis with the indicated antibodies.

    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    ZSTK474 is an ATP-competitive pan-class I PI3K inhibitor with IC50s of 16 nM, 44 nM, 4.6 nM and 49 nM for PΙ3Κα, PI3Kβ, PI3Kδ and PI3Kγ, respectively.

    IC50 & Target[2]

    PI3Kδ

    4.6 nM (IC50)

    PI3Kα

    16 nM (IC50)

    PI3Kβ

    44 nM (IC50)

    PI3Kγ

    49 nM (IC50)

    Autophagy

     

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HCT-116 IC50
    1.31 μM
    Compound: ZSTK474
    Antiproliferative activity against human HCT116 cells after 72 hrs by CCK-8 assay
    Antiproliferative activity against human HCT116 cells after 72 hrs by CCK-8 assay
    		[PMID: 30245395]
    HCT-116 IC50
    1.31 μM
    Compound: ZSTK474
    Antiproliferative activity against human HCT116 cells harboring PI3Kalpha H1047R mutant after 72 hrs by CCK8 assay
    Antiproliferative activity against human HCT116 cells harboring PI3Kalpha H1047R mutant after 72 hrs by CCK8 assay
    		[PMID: 30071408]
    HCT-116 IC50
    78 nM
    Compound: 1, ZSTK474
    Inhibition of PIK3CA H1047R mutant-mediated cell signaling in human HCT116 cells expressing PTEN assessed as inhibition of insulin-induced pAkt/PKB phosphorylation at Thr308 treated for 15 mins before insulin challenge measured after 5 mins by immunoblott
    Inhibition of PIK3CA H1047R mutant-mediated cell signaling in human HCT116 cells expressing PTEN assessed as inhibition of insulin-induced pAkt/PKB phosphorylation at Thr308 treated for 15 mins before insulin challenge measured after 5 mins by immunoblott
    		[PMID: 21882832]
    HCT-116 IC50
    97 nM
    Compound: 1, ZSTK474
    Inhibition of PIK3CA H1047R mutant-mediated cell signaling in human HCT116 cells expressing PTEN assessed as inhibition of insulin-induced pAkt/PKB phosphorylation at Ser473 treated for 15 mins before insulin challenge measured after 5 mins by immunoblott
    Inhibition of PIK3CA H1047R mutant-mediated cell signaling in human HCT116 cells expressing PTEN assessed as inhibition of insulin-induced pAkt/PKB phosphorylation at Ser473 treated for 15 mins before insulin challenge measured after 5 mins by immunoblott
    		[PMID: 21882832]
    HT-29 GI50
    300 nM
    Compound: ZSTK474
    Antiproliferative activity against human HT-29 cells incubated for 3 days by WST8 assay
    Antiproliferative activity against human HT-29 cells incubated for 3 days by WST8 assay
    		[PMID: 33284613]
    LNCaP IC50
    210 nM
    Compound: 6
    Antiproliferative activity against human LNCAP cells after 3 days by MTS assay
    Antiproliferative activity against human LNCAP cells after 3 days by MTS assay
    		[PMID: 20227881]
    MCF7 IC50
    5.27 μM
    Compound: ZSTK474
    Antiproliferative activity against human MCF7 cells after 72 hrs by CCK-8 assay
    Antiproliferative activity against human MCF7 cells after 72 hrs by CCK-8 assay
    		[PMID: 30245395]
    MCF7 IC50
    5.27 μM
    Compound: ZSTK474
    Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay
    		[PMID: 30071408]
    MDA-MB-468 EC50
    3.2 μM
    Compound: ZSTK474
    Cytotoxicity against PTEN-deficient human MDA-MB-468 cells assessed as inhibition of cell growth after 48 hrs by Cell Titer 96 assay
    Cytotoxicity against PTEN-deficient human MDA-MB-468 cells assessed as inhibition of cell growth after 48 hrs by Cell Titer 96 assay
    		[PMID: 23795239]
    Sf21 IC50
    0.003 μM
    Compound: 4a, ZSTK474
    Inhibition of PI3Kdelta (unknown origin) expressed in SF21 cells using phosphatidylinositol as substrate after 60 mins by Kinase-Glo assay
    Inhibition of PI3Kdelta (unknown origin) expressed in SF21 cells using phosphatidylinositol as substrate after 60 mins by Kinase-Glo assay
    		[PMID: 23265896]
    Sf21 IC50
    0.006 μM
    Compound: 4a, ZSTK474
    Inhibition of PI3Kbeta (unknown origin) expressed in SF21 cells using phosphatidylinositol as substrate after 60 mins by Kinase-Glo assay
    Inhibition of PI3Kbeta (unknown origin) expressed in SF21 cells using phosphatidylinositol as substrate after 60 mins by Kinase-Glo assay
    		[PMID: 23265896]
    Sf21 IC50
    0.006 μM
    Compound: 4a, ZSTK474
    Inhibition of PI3Kalpha (unknown origin) expressed in SF21 cells using phosphatidylinositol as substrate after 60 mins by Kinase-Glo assay
    Inhibition of PI3Kalpha (unknown origin) expressed in SF21 cells using phosphatidylinositol as substrate after 60 mins by Kinase-Glo assay
    		[PMID: 23265896]
    Sf21 IC50
    0.038 μM
    Compound: 4a, ZSTK474
    Inhibition of PI3Kgamma (unknown origin) expressed in SF21 cells using phosphatidylinositol as substrate after 60 mins by Kinase-Glo assay
    Inhibition of PI3Kgamma (unknown origin) expressed in SF21 cells using phosphatidylinositol as substrate after 60 mins by Kinase-Glo assay
    		[PMID: 23265896]
    Sf21 IC50
    6 nM
    Compound: ZSTK-47
    Inhibition of PI3Kbeta (unknown origin) expressed in Escherichia coli-infected fall armyworm sf21 cells co-expressing p85 by kinase-glo luminescence assay
    Inhibition of PI3Kbeta (unknown origin) expressed in Escherichia coli-infected fall armyworm sf21 cells co-expressing p85 by kinase-glo luminescence assay
    		[PMID: 27387421]
    U-87MG ATCC IC50
    111 nM
    Compound: 1, ZSTK474
    Inhibition of PIK3CA-mediated cell signaling in PTEN-deficient human U87MG cells assessed as inhibition of insulin-induced pAkt/PKB phosphorylation at Ser473 treated for 15 mins before insulin challenge measured after 5 mins by immunoblotting
    Inhibition of PIK3CA-mediated cell signaling in PTEN-deficient human U87MG cells assessed as inhibition of insulin-induced pAkt/PKB phosphorylation at Ser473 treated for 15 mins before insulin challenge measured after 5 mins by immunoblotting
    		[PMID: 21882832]
    U-87MG ATCC IC50
    32 nM
    Compound: 1, ZSTK474
    Inhibition of PIK3CA-mediated cell signaling in PTEN-deficient human U87MG cells assessed as inhibition of insulin-induced pAkt/PKB phosphorylation at Thr308 treated for 15 mins before insulin challenge measured after 5 mins by immunoblotting
    Inhibition of PIK3CA-mediated cell signaling in PTEN-deficient human U87MG cells assessed as inhibition of insulin-induced pAkt/PKB phosphorylation at Thr308 treated for 15 mins before insulin challenge measured after 5 mins by immunoblotting
    		[PMID: 21882832]
    體外研究
    (In Vitro)

    Lineweaver-Burk plot analysis revealed that ZSTK474 inhibits all four PI3K isoforms in an ATP-competitive manner. The Ki values determined for the four PI3K isoforms showed that ZSTK474 inhibited the PI3Kδ isoform most effectively with a Ki of 1.8 nM, whereas the other isoforms are inhibited with 4-10-fold higher Ki values. Therefore, ZSTK474 should be regarded as a pan-PI3K inhibitor. We also determined the IC50 values for inhibiting the four PI3K isoforms with ZSTK474 and LY294002. The IC50 values of ZSTK474 (16, 44, 4.6 and 49 nM for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively) are shown to be consistent with the Ki values (6.7, 10.4, 1.8 and 11.7 nM for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively), which further supported the idea that ZSTK474 inhibits PI3Kδ most potently. Even at a concentration of 100 μM, ZSTK474 inhibits mTOR activity rather weakly[1].

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

    In mice subjected to MCAO, treatment with ZSTK474 is tested at dosages of 50, 100, 200, and 300 mg/kg. Since the 200 mg/kg dose produces significant improvement and no obvious toxic effects (P<0.01), mice are treated with ZSTK474 at a dose of 200 mg/kg/day daily for three post-MCAO days during the remaining experiments of this study. Neurological function is examined in mice suffered from MCAO followed by 24, 48, and 72 h of reperfusion. In the ZSTK474 group, neurological function scores are significantly better than the control group except the corner test[2].

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

    417.41

    Formula

    C19H21F2N7O2
    CAS 號
    性狀

    固體

    顏色

    White to off-white

    運輸條件

    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)胞實驗： 

    DMSO 中的溶解度 : 33.33 mg/mL (79.85 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 2.3957 mL 11.9786 mL 23.9573 mL
    5 mM 0.4791 mL 2.3957 mL 4.7915 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，請在2年內(nèi)使用， -20°C儲存時，請在1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

    動物實驗：

    以下溶解方案源自文獻(xiàn)，僅供參考，建議您先取少量樣品進(jìn)行嘗試。

    • 方案 一

      ZSTK474 is suspended in 5% hydroxypropyl cellulose[3].

    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    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
    由于實驗過程有損耗，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: 99.88%

    參考文獻(xiàn)
    Kinase Assay
    [1]

    The linear phase of each kinetic reaction is defined at the respective enzyme amount (0.05, 0.1, 0.12 and 1 μg/mL for PI3Kα, PI3β, PI3δ and PI3γ, respectively) and reaction time (20 min). PI3K activity is assayed at various concentrations of ATP (5, 10, 25, 50, 100 μM) in the presence of increasing concentrations of ZSTK474. A Lineweaver-Burk plot is developed by plotting 1/v (the inverse of v, where v is obtained by subtracting the HTRF signal of the kinase test sample from the HTRF signal of the minus-enzyme control) versus 1/[ATP] (the inverse of the ATP concentration). For the minus-enzyme control, PIP2 is incubated with ATP in the absence of kinase. To determine the Ki value (inhibition constant) of ZSTK474 for each PI3K isoform, the slope of the respective Lineweaver-Burk plot is replotted against the ZSTK474 concentration. The Ki values are calculated by analysis using GraphPad Prism 4[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Mice[2]
    Mice are randomly assigned to receive different doses of ZSTK474 (50, 100, 200, and 300 mg/kg) to determine the optimum dose; in our experiment, the optimum dose is 200 mg/kg. Then mice are randomly assigned to one of three groups: a sham-operated group (phosphate-buffered saline, PBS); a control group (MCAO+PBS); a ZSTK474-treated group (MCAO+ZSTK474). In the ZSTK474-treated group, the mice are given the optimum dose of 200 mg/kg ZSTK474. In the sham-operated group and control group, mice are given an equivalent volume of PBS. All mice receive that same dose daily via oral gavage beginning at 6 h after the onset of focal ischemia and continuing for two more days, i.e., for a total of 3 days.

    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，請在2年內(nèi)使用， -20°C儲存時，請在1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 2.3957 mL 11.9786 mL 23.9573 mL 59.8932 mL
    5 mM 0.4791 mL 2.3957 mL 4.7915 mL 11.9786 mL
    10 mM 0.2396 mL 1.1979 mL 2.3957 mL 5.9893 mL
    15 mM 0.1597 mL 0.7986 mL 1.5972 mL 3.9929 mL
    20 mM 0.1198 mL 0.5989 mL 1.1979 mL 2.9947 mL
    25 mM 0.0958 mL 0.4791 mL 0.9583 mL 2.3957 mL
    30 mM 0.0799 mL 0.3993 mL 0.7986 mL 1.9964 mL
    40 mM 0.0599 mL 0.2995 mL 0.5989 mL 1.4973 mL
    50 mM 0.0479 mL 0.2396 mL 0.4791 mL 1.1979 mL
    60 mM 0.0399 mL 0.1996 mL 0.3993 mL 0.9982 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：
    ZSTK474
    目錄號：
    HY-50847
    需求量：