2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Stem Cell/Wnt Epigenetics Autophagy
  3. EGFR STAT JAK Autophagy
  4. AG490

AG490  (Synonyms: Tyrphostin AG490; Tyrphostin B42)

目录号: HY-12000 纯度: 99.97%
COA 产品使用指南

摩尔计算器

AG490 (Tyrphostin AG490) 是酪氨酸激酶抑制剂，其抑制EGFR，Stat-3 和 JAK2/3。

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AG490 Chemical Structure

AG490 Chemical Structure

CAS No. : 133550-30-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥500
In-stock
5 mg ￥232
In-stock
10 mg ￥371
In-stock
50 mg ￥1200
In-stock
100 mg ￥1800
In-stock
200 mg ￥2813
In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of AG490:

AG490 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 98 篇科研文献

WB
IF

    AG490 purchased from MCE. Usage Cited in: Cell Death Dis. 2019 Jun 13;10(6):465.  [Abstract]

    pcDNA-AQP3 is used to upregulated AQP3 expression. We found AQP3 overexpression had no influence on STAT3 expression, but could promote STAT3 activation. AG-490 treatment could inhibit STAT3 activation and eliminate the influence of AQP3 overexpression.

    AG490 purchased from MCE. Usage Cited in: Front Cell Dev Biol. 2019 Nov 1;7:253.  [Abstract]

    STAT3 regulates miR-384 transcription. CD4C naïve T cells are cultured with IL-6, siRNA, or AG490, and then p-STAT3 and STAT3 levels are tested by Western blot.

    AG490 purchased from MCE. Usage Cited in: J Ethnopharmacol. 2019 Mar 25;232:62-72.  [Abstract]

    After incubation with AG490 (50 μM), RP (40 μg/mL) or both for 24 h, total protein from SMMC-7721s are analyzed by Western blot.

    AG490 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Aug 29;9(9):867.  [Abstract]

    AG490 decreases c-Met expression in MGC803 and AGS cells when they are co-cultured with CAFs.

    AG490 purchased from MCE. Usage Cited in: J Agric Food Chem. 2018 Nov 7;66(44):11757-11766.  [Abstract]

    The number of GFP-LC3 dots are reduced significantly after inhibiting STAT3 (AG-490) signaling.

    AG490 purchased from MCE. Usage Cited in: Transl Oncol. 2018 Dec 26;12(3):485-492.   [Abstract]

    AG490 blocks the IL6/STAT3/PD-L1 signaling pathway and is more pronounced after knockdown of IDO1. T24 and UMUC3 cells after IDO1 knockdown are treated with STAT3 specific inhibitor AG490. The protein levels of STAT3, P-STAT3, and PD-L1 are measured by Western blot analysis.

    AG490 purchased from MCE. Usage Cited in: Reprod Biol Endocrinol. 2018 May 31;16(1):55.  [Abstract]

    Western blot analysis of claudin 5, occludin and ZO-1 in TM4 cells, cells are treated with 100 nM Leptin or pre-treated with different inhibitors following a 100 nM Leptin treatment.

    AG490 purchased from MCE. Usage Cited in: Mol Med Rep. 2018 Jun;17(6):7595-7602.  [Abstract]

    Representative images show the expression levels of α SMA, calponin and osteopontin (OPN) protein.

    AG490 purchased from MCE. Usage Cited in: Reprod Sci. 2019 Jun;26(6):829-838.  [Abstract]

    The protein expression levels of p-JAK2, JAK2, p-STAT3, and STAT3 are detected by Western blot with the treatment of ,MSA, AG490 or MSA+AG490.

    AG490 purchased from MCE. Usage Cited in: Oncogene. 2017 May 25;36(21):2946-2956.  [Abstract]

    (a) Immunoblotting analysis of pSTAT3, CITED4, and CCND1 in CL1-5 cells treated with AG490 (5 μM) for the indicated times. α-Tubulin is assessed as an internal control. (b) Q-PCR analysis of CITED4 in A549 cells treated with AG490 (5 μM) for the indicated times.

    AG490 purchased from MCE. Usage Cited in: Mol Med Rep. 2017 Dec;16(6):9309-9316.  [Abstract]

    Ad IL 23 intensifies the high expression levels of IL 17A, TNF α and IL 6 induced by myocardial I/R, which is inhibited by AG490. Levels of IL 17A in myocardial tissues from infarct and risk regions (n=6). The addition of AG490 significantly inhibits the effect of Ad IL 23.

    查看 EGFR 亚型特异性产品:

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    EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

    查看 STAT 亚型特异性产品:

    查看所有亚型
    STAT3 STAT5 STAT6 STAT1

    查看 JAK 亚型特异性产品:

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    JAK1 JAK2 JAK3 Tyk2 JAK

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    AG490 (Tyrphostin AG490) is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.

    IC50 & Target[1]

    EGFR

     

    Stat-3

     

    体外研究
    (In Vitro)

    AG490 inhibits the activation of Stat-3 by selectively blocking JAK2. AG490 is used to selectively inhibit JAK/Stat-3 activation. At a dose of 10 μM, Stat-3 phosphorylation is decreased by >95% and cell viability is maintained. AG490 at a dose of 10 μM results in >95% decrease in pStat-3 in EGF-stimulated A431 cells with no effect on Stat-3 mass[1]. AG-490 is a potent inhibitor of the JAK3/STAT, JAK3/AP-1, and JAK3/MAPK pathways and their cellular consequences. AG-490 abolishes IL-2-inducible [3H]thymidine incorporation in a dose-dependent manner, displaying an IC50 of 25 μM. AG-490 potently inhibits IL-2-mediated proliferation in T cells, results distinct from previous studies that showed this agent induced apoptosis in ALL cells while exerting apparently no effects on the growth of mitogen-stimulated normal T cells[2].

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

    AG490 相关抗体:
    体内研究
    (In Vivo)

    AG490 significantly inhibits the development of type 1 diabetes (T1D) (p = 0.02, p = 0.005; at two different time points). Monotherapy of newly diagnosed diabetic NOD mice with AG490 (1 mg/mouse) markedly results in disease remission in treated animals (n=23) in comparision to the absolute inability (0%; 0/10, p=0.003, Log-rank test) of DMSO and sustained eugluycemia is maintained for several months following drug withdrawal[3]. AG490 (1-10 µg) significantly attenuates ʎ-carrageenan-induced thermal hyperalgesia in a dose-dependent manner. AG490 also reduces mechanical hyperalgesia[4].

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

    294.30

    Formula

    C17H14N2O3
    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
    In Vitro: 

    DMSO 中的溶解度 : ≥ 50 mg/mL (169.89 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 3.3979 mL 16.9895 mL 33.9789 mL
    5 mM 0.6796 mL 3.3979 mL 6.7958 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

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (7.07 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (7.07 mM); 悬浊液; 超声助溶

      此方案可获得 2.08 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

      以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
    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
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.97%

    COA (189 KB) HNMR (253 KB) LCMS (264 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [1]

    A colorimetric cell proliferation assay is performed using the CellTiter 96 kit. Briefly, A431 cells are plated in 96-well plates (2000 cells/well) and cultured in DMEM/HAM's F-12 supplemented with 10% FCS for 24 h. Cells are incubated in serum-free media for 24 h. EGF (10 ng/mL) is added to all wells. Tyrphostin AG1478 (0.25 mM) and AG490 (10 mM) are added alone or in combination and the culture is incubated for the appropriate time. Medium is aspirated and CellTiter 96 Aqueous One Solution Reagent (20 μL) is added to each well. The plates are incubated at 37°C for up to 1 h and absorbance recorded at 490 nm using a 96-well plate reader. Data are derived from at least three independent experiments (in triplicate) for the both single agents and combination studies. IC50 values for Tyrphostin AG1478 (EGFR inhibitor) and AG490 (JAK/STAT inhibitor) are determined. The growth inhibitory effects of the combination are quantified using the Calucsyn software program[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3][4]

    Mice[3]
    Female NOD/LtJ, NOD.Scid, and BALB/c mice are used. One vial of compound containing 5 mg of AG490 is injected into5 mice (1 mg/mouse) via the i.p route. The control groups are receive the same volume of the vehicle under the same regimens and conditions.
    Rats[4]
    A total of 28 Male Sprague-Dawley rats (250-300 g) are used. The experiments are performed in rats 48 h after ʎ-carrageenan injection. A total of 4 groups (n=6) of rats are randomly included in the dose-response study. Group 1 is the vehicle control, which receive 100 µL i.pl. injection of 3.5% DMSO in saline. Groups 2-4 are injected with 3 different doses of AG490 (1, 5 or 10 µg). To study the effects of naloxone on AG490-induced antinociception, an additional group of rats (group 5; n=4) is observed. Group 5 is co-administered with AG490 (10 µg) and Naloxone (10 µg). The drugs are administered i.pl. in a volume of 100 µl. As reported earlier, the in vivo pharmacological effects of AG490 are observed 4 h after treatment. Thus, the behavioral tests are performed before (baseline assessment) and 4 h after treatment. First, the rats are subjected to the thermal hyperalgesia test; 10 min later, the paw pressure test is performed on the same set of rats. All the experiments are performed between 8:00 a.m. and 2:00 p.m. to reduce the confounding influence of diurnal variations, and all the procedures are performed in a blinded fashion.

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

    AG490 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 3.3979 mL 16.9895 mL 33.9789 mL 84.9473 mL
    5 mM 0.6796 mL 3.3979 mL 6.7958 mL 16.9895 mL
    10 mM 0.3398 mL 1.6989 mL 3.3979 mL 8.4947 mL
    15 mM 0.2265 mL 1.1326 mL 2.2653 mL 5.6632 mL
    20 mM 0.1699 mL 0.8495 mL 1.6989 mL 4.2474 mL
    25 mM 0.1359 mL 0.6796 mL 1.3592 mL 3.3979 mL
    30 mM 0.1133 mL 0.5663 mL 1.1326 mL 2.8316 mL
    40 mM 0.0849 mL 0.4247 mL 0.8495 mL 2.1237 mL
    50 mM 0.0680 mL 0.3398 mL 0.6796 mL 1.6989 mL
    60 mM 0.0566 mL 0.2832 mL 0.5663 mL 1.4158 mL
    80 mM 0.0425 mL 0.2124 mL 0.4247 mL 1.0618 mL
    100 mM 0.0340 mL 0.1699 mL 0.3398 mL 0.8495 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:

    AG490133550-30-8Tyrphostin AG490 Tyrphostin B42AG 490AG-490Tyrphostin AG 490Tyrphostin AG-490Tyrphostin B42Tyrphostin B 42Tyrphostin B-42EGFRSTATJAKAutophagyEpidermal growth factor receptorErbB-1HER1Janus kinaseInhibitorinhibitorinhibit

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