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  2. Protein Tyrosine Kinase/RTK Apoptosis
  3. IGF-1R Insulin Receptor Apoptosis
  4. GSK1904529A

GSK1904529A 是一種有效的，選擇性的，具有口服活性和 ATP 競(jìng)爭(zhēng)性的胰島素樣生長(zhǎng)因子 1 受體 (IGF-1R) 和胰島素受體 (IR) 抑制劑，IC50 值分別為 27 和 25 nM。GSK1904529A 在其他 45 種絲氨酸/蘇氨酸和酪氨酸激酶中顯示出較弱的活性 (IC50>1 μM)。GSK1904529A 具有抗腫瘤活性。

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GSK1904529A Chemical Structure

GSK1904529A Chemical Structure

CAS No. : 1089283-49-7

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1270
In-stock
5 mg ￥843
In-stock
10 mg ￥1350
In-stock
50 mg ￥3450
In-stock
100 mg 現(xiàn)貨 詢價(jià)
200 mg   詢價(jià)  
500 mg   詢價(jià)  

* Please select Quantity before adding items.

    GSK1904529A purchased from MCE. Usage Cited in: Clin Cancer Res. 2014 Nov 1;20(21):5483-95.  [Abstract]

    Effects of GSK1904529A as single agents, respectively, on mediators of IGF-1R- and ERK1/ERK2-signaling pathways.(A-B) Effect of GSK1904529A on phosphorylation of IGF-1R (A) and Erk1/Erk2 (B).

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    GSK1904529A is a potent, selective, orally active, and ATP-competitive inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR), with IC50s of 27 and 25 nM, respectively. GSK1904529A shows poor activity (IC50>1 μM) in 45 other serine/threonine and tyrosine kinases. GSK1904529A exhibits anti-tumor activity[1][2].

    IC50 & Target

    IC50: 27 nM (IGF-1R), 25 nM (IR)[1]
    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    > 20000 nM
    Compound: 24
    Antiproliferative activity against human A549 cells after 72 hrs by Celltiter assay
    Antiproliferative activity against human A549 cells after 72 hrs by Celltiter assay
    		[PMID: 19101143]
    COLO 205 IC50
    124 nM
    Compound: 24
    Antiproliferative activity against human COLO205 cells after 72 hrs by Celltiter assay
    Antiproliferative activity against human COLO205 cells after 72 hrs by Celltiter assay
    		[PMID: 19101143]
    HFF IC50
    > 20000 nM
    Compound: 24
    Antiproliferative activity against HFF cells after 72 hrs by Celltiter assay
    Antiproliferative activity against HFF cells after 72 hrs by Celltiter assay
    		[PMID: 19101143]
    LP-1 IC50
    104 nM
    Compound: 24
    Antiproliferative activity against human LP-1 cells after 72 hrs by Celltiter assay
    Antiproliferative activity against human LP-1 cells after 72 hrs by Celltiter assay
    		[PMID: 19101143]
    NCI-H929 IC50
    81 nM
    Compound: 24
    Antiproliferative activity against human NCI-H929 cells after 72 hrs by Celltiter assay
    Antiproliferative activity against human NCI-H929 cells after 72 hrs by Celltiter assay
    		[PMID: 19101143]
    體外研究
    (In Vitro)

    GSK1904529A displays high affinities for IGF-1R and IR, with Kis of 1.6 and 1.3 nM, respectively[1].
    GSK1904529A (72 h) inhibits tumor cells proliferation with IC50s ranges from 35 nM to >30 μM, and Ewing's sarcoma and multiple myeloma cell lines are greatest sensitive[1].
    GSK1904529A (0.03-3 μM; 24 and 48 h) arrests cells at the G1 phase of the cell cycle[1].
    GSK1904529A (2 h) inhibits phosphorylation of IGF-IR and IR with IC50s of 22 and 19 nM in NIH-3T3/LISN and NIH-3T3-hIR cells, respectively[1].
    GSK1904529A (0.01-3 μM; 4 h) blocks the major downstream signal transduction pathways mediated by IGF-IR and IR in NIH-3T3/LISN and NIH-3T3-hIR cells[1].

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

    Cell Cycle Analysis[1]

    Cell Line: COLO 205, MCF-7, and NCI-H929 cells
    Concentration: 0, 0.03, 0.1, 0.3, 1, 3 μM
    Incubation Time: 24 and 48 hours
    Result: Increased the accumulation in G1 and decreased accumulation in S and G2-M phases of the cell cycle.

    Western Blot Analysis[1]

    Cell Line: NIH-3T3/LISN and NIH-3T3-hIR cells
    Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3 μM
    Incubation Time: 4 hours
    Result: Inhibited the ligand-induced phosphorylation of IGF-IR and IR at concentrations >0.01 μM.
    Decreased the phosphorylation of AKT, IRS-1, and ERK.
    體內(nèi)研究
    (In Vivo)

    GSK1904529A (30 mg/kg; p.o. once or twice daily for 21 d) has antitumor activity in mice[1].
    GSK1904529A (1-30 mg/kg; a single p.o.) decreases IGF-I-induced IGF-IR phosphorylation in a dose-dependent manner in mice[1].
    GSK1904529A (30 mg/kg; p.o. once or twice daily for 21 d) has no significant alterations in the blood glucose levels in mice[1].

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

    Animal Model: Female athymic nu/nu CD-1 mice are bring NIH-3T3/LISN tumor[1]
    Dosage: 30 mg/kg
    Administration: P.o. once or twice daily for 21 d
    Result: Resulted in 56% (once daily) and 98% (twice daily) inhibition of tumor growth.
    No significant decrease in body weight on the once-daily schedule.
    Observed 11-13% of body weight loss, and recovered to near baseline 6 days after the cessation of treatment in twice-daily group.
    分子量

    851.96

    Formula

    C44H47F2N9O5S
    CAS 號(hào)
    性狀

    固體

    顏色

    Light yellow to yellow

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)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 : 50 mg/mL (58.69 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 1.1738 mL 5.8688 mL 11.7376 mL
    5 mM 0.2348 mL 1.1738 mL 2.3475 mL
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)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(dòng)物實(shí)驗(yàn)：

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.75 mg/mL (3.23 mM); 澄清溶液

      此方案可獲得 ≥ 2.75 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 27.5 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
    請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
    請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料
    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?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 1.1738 mL 5.8688 mL 11.7376 mL 29.3441 mL
    5 mM 0.2348 mL 1.1738 mL 2.3475 mL 5.8688 mL
    10 mM 0.1174 mL 0.5869 mL 1.1738 mL 2.9344 mL
    15 mM 0.0783 mL 0.3913 mL 0.7825 mL 1.9563 mL
    20 mM 0.0587 mL 0.2934 mL 0.5869 mL 1.4672 mL
    25 mM 0.0470 mL 0.2348 mL 0.4695 mL 1.1738 mL
    30 mM 0.0391 mL 0.1956 mL 0.3913 mL 0.9781 mL
    40 mM 0.0293 mL 0.1467 mL 0.2934 mL 0.7336 mL
    50 mM 0.0235 mL 0.1174 mL 0.2348 mL 0.5869 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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    產(chǎn)品名稱：
    GSK1904529A
    目錄號(hào)：
    HY-10524
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