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  2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Anti-infection
  3. EGFR HCV Influenza Virus
  4. AG-1478

AG-1478  (Synonyms: Tyrphostin AG-1478; NSC 693255)

目錄號(hào): HY-13524 純度: 99.22%
COA 產(chǎn)品使用指南 技術(shù)支持

AG-1478 (Tyrphostin AG-1478) 是一種選擇性的 EGFR 酪氨酸激酶抑制劑，IC50 為 3 nM。AG-1478 對(duì) HCV 和腦心肌炎病毒 (EMCV) 具有抗病毒作用。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

AG-1478 Chemical Structure

AG-1478 Chemical Structure

CAS No. : 153436-53-4

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥550
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5 mg ￥500
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10 mg ￥700
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50 mg ￥2495
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100 mg ￥3500
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200 mg   詢(xún)價(jià)  
500 mg   詢(xún)價(jià)  

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Customer Review

Other Forms of AG-1478:

MCE 顧客使用本產(chǎn)品發(fā)表的 38 篇科研文獻(xiàn)

WB

    AG-1478 purchased from MCE. Usage Cited in: Environ Toxicol. 2023 Feb 9.  [Abstract]

    AG1478 (2 μM) suppresses the phosphorylation of EGFR and ERK1/2 and subsequently upregulates the expression of ZO-1 and occludin in BEAS-2B cells.

    AG-1478 purchased from MCE. Usage Cited in: Sci Rep. 2017 Jan 19;7:40802.  [Abstract]

    EGFR participates the process of ACh induced cell proliferation and signaling transduction. After adding 10?μM EGFR specific inhibitor AG1478 2?h prior to ACh addition, protein changes are analyzed by western blot.

    • 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

    AG-1478 (Tyrphostin AG-1478) is a selective EGFR tyrosine kinase inhibitor with IC50 of 3 nM. AG-1478 has antiviral effects against HCV and encephalomyocarditis virus (EMCV).

    IC50 & Target[1][4]

    EGFR

    3 nM (IC50)

    HCV

     

    EMCV

     

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A-431 IC50
    0.31 nM
    Compound: 31
    Concentration required to inhibit the phosphorylation of a 14-residue fragment of phospholipase C gamma 1 by Epidermal growth factor receptor from A431 cell vesicles
    Concentration required to inhibit the phosphorylation of a 14-residue fragment of phospholipase C gamma 1 by Epidermal growth factor receptor from A431 cell vesicles
    		[PMID: 8568816]
    體外研究
    (In Vitro)

    AG-1478 (AG1478) is irreversible for growth regulation of human lung (A549) and prostate (DU145) cancer cell lines, cultured in chemically defined DMEM/F12 medium. AG-1478 seems to be more effective at lower concentrations, but is unable to completely inhibit growth of A549 cells[1]. Inhibition of EGFR by specific tyrosine kinase inhibitor AG-1478 (AG1478) significantly decreases the angiotensin II-mediated synthesis of TGF-β and fibronectin by cardiac fibroblasts. EGFR is pharmacologically inhibited by small-molecule inhibitor AG-1478 with IC50 of 4 nM[2]. Both Polyfect (PF) and Superfect (SF) treatment lead to increased apoptosis in HEK 293 cells to a similar extent as assessed by flow cytometry. The antioxidant, tempol, significantly reduced dendrimer-mediated apoptosis for both PF and SF. AG-1478 (AG1478), at a 10-fold higher dose (100 μM) than used in signaling studies, is used as a positive control and significantly induced apoptosis in HEK 293 cells[3].

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

    Administration of AG-1478 (AG1478) significantly reduces myocardial inflammation, fibrosis, apoptosis, and dysfunction in both two obese mouse models. ApoE-/- mice are first fed with HFD for 8 weeks (ApoE-HFD), and then administrated with AG-1478 (10 mg/kg/day) or 542 (10 mg/kg/day) for another 8 weeks by oral gavage. AG-1478 or 542 treatment blocks HFD induced cardiac EGFR phosphorylation in vivo, without affecting the plasma level of low density lipoprotein (LDL) and total triglyceride (TG)[2]. Administration of EGF (10 nM) leads to a robust and reproducible elevation in EGFR phosphorylation that can be blocked by AG-1478 (AG1478), a known inhibitor of EGFR phosphorylation. Increasing doses of Polyfect (PF) result in a significant reduction in EGF-induced EGFR phosphorylation (p<0.05) but this is to a lesser extent than observed with AG1478[3].

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

    315.75

    Formula

    C16H14ClN3O2
    CAS 號(hào)
    性狀

    固體

    顏色

    White to off-white

    中文名稱(chēng)

    酪氨酸磷酸化抑制劑 AG-1478
    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 (158.35 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(kāi)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 3.1671 mL 15.8353 mL 31.6706 mL
    5 mM 0.6334 mL 3.1671 mL 6.3341 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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)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: ≥ 2.08 mg/mL (6.59 mM); 澄清溶液

      此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 20.8 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。
    • 方案 二

      請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (6.59 mM); 澄清溶液

      此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。

    以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶。

    • 方案 一

      請(qǐng)依序添加每種溶劑： 1% CMC/0.5% Tween-80 in Saline water

      Solubility: 5 mg/mL (15.84 mM); 懸濁液; 超聲助溶

    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(guò)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(guò) 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
    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(guò)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(guó)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(guò)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

    純度: 99.22%

    參考文獻(xiàn)
    Cell Assay
    [1]

    DU145 (HTB-81) and A549 (CCL-185) cells are seeded on 96-well plates at concentrations of 4×103 cells/well in MEM (DU145 cells) or DMEM (A549 cells). Following 24 h of incubation, the culture medium is replaced with serum-free DMEM/F12 (1:1) supplemented with Transferrin (5 mg/mL), sodium selenite (2 ng/mL) and albumin (0.5 mg/mL) [DMEM/F12+]. After an additional 24 h of incubation (Day 0), the medium is replaced by serum-free DMEM/F12+ medium containing tyrosine kinase inhibitors: AG494, AG-1478 respectively in concentration ranges 1-20 μM and 0.1-8 μM. The incubation is continued for the next 24 h at 37°C in a humidified atmosphere. The modified crystal violet staining method (CV) and MTT assay are used to determine the influence of the tyrphostins on the proliferation of target cells. The absorbance is measured using a Tecan multiscan plate recorder[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2][3]

    Mice[2]
    28 C57BL/6 or ApoE-/- mice are randomly divided into four weight-matched groups. 7 mice are fed with standard animal low-fat diet containing 10 kcal.% fat, 20 kcal.% protein and 70 kcal.% carbohydrate serve as a normal control group (Control or ApoE-LF), while the remaining 21 mice are fed with high-fat diet containing 60 kcal.% fat, 20 kcal.% protein and 20 kcal.% carbohydrate for 16 weeks. Since 9th week, AG-1478 or 542 are given daily by oral gavage at a dose of 10 mg/kg/day for the next 8 weeks. Mice in the Control and HFD groups are gavaged with vehicle (1% CMC-Na solution) only. At the day before the sacrifice of ApoE-/- mice, doppler analysis is performed to determine the pathologic cardiac hypertrophy.
    Rats[3]
    Male Wistar rats weighing about 300g are used in this study and divided into the following groups (N=5). Group 1: Non-diabetic (Control, C) animals, Group 2: C+PF (10mg/kg administered as a single intraperotoneal (i.p) injection) Group 3: C+SF (10mg/kg i.p); Group 4: C+AG-1478 (1 mg/kg i.p). Group 5: Rats bearing 4 weeks of diabetes (D) induced by a single i.p. injection of streptozotocin (55 mg/kg body weight); Group 6: D+PF (10 mg/kg i.p) Group 7: D+SF (10 mg/kg i.p) and Group 8: D+AG-1478 (1 mg/kg i.p). AG-1478 and dendrimer treatments are administered as single dose for 24h prior to sacrifice. Rat body weight and basal glucose levels are assessed before and after treatments just before sacrificing the animals. An automated blood glucose analyzer is used to assess blood glucose concentrations and rats with a blood glucose concentration above 250 mg/dL (approx. 14 mM) are declared diabetic as in previous studies.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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 3.1671 mL 15.8353 mL 31.6706 mL 79.1766 mL
    5 mM 0.6334 mL 3.1671 mL 6.3341 mL 15.8353 mL
    10 mM 0.3167 mL 1.5835 mL 3.1671 mL 7.9177 mL
    15 mM 0.2111 mL 1.0557 mL 2.1114 mL 5.2784 mL
    20 mM 0.1584 mL 0.7918 mL 1.5835 mL 3.9588 mL
    25 mM 0.1267 mL 0.6334 mL 1.2668 mL 3.1671 mL
    30 mM 0.1056 mL 0.5278 mL 1.0557 mL 2.6392 mL
    40 mM 0.0792 mL 0.3959 mL 0.7918 mL 1.9794 mL
    50 mM 0.0633 mL 0.3167 mL 0.6334 mL 1.5835 mL
    60 mM 0.0528 mL 0.2639 mL 0.5278 mL 1.3196 mL
    80 mM 0.0396 mL 0.1979 mL 0.3959 mL 0.9897 mL
    100 mM 0.0317 mL 0.1584 mL 0.3167 mL 0.7918 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(chēng)：
    AG-1478
    目錄號(hào)：
    HY-13524
    需求量：