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  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)

目錄號(hào): HY-12000 純度: 99.92%
COA 產(chǎn)品使用指南 技術(shù)支持

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

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)

AG490 Chemical Structure

AG490 Chemical Structure

CAS No. : 133550-30-8

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規(guī)格 價(jià)格 是否有貨 數(shù)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   詢價(jià)  
1 g   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of AG490:

MCE 顧客使用本產(chǎn)品發(fā)表的 131 篇科研文獻(xiàn)

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: 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: Front Cell Dev Biol. 2019 Nov 1;7:253.  [Abstract]

    STAT3 regulates miR-384 transcription. CD4C na?ve 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: 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 亞型特異性產(chǎn)品:

    查看 STAT 亞型特異性產(chǎn)品:

    查看 JAK 亞型特異性產(chǎn)品:

    • 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

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

    IC50 & Target[1]

    EGFR

     

    Stat-3

     

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HeLa IC50
    > 100 μM
    Compound: AG-490
    Cytotoxicity against human HeLa cells after 48 hrs by MTT assay
    Cytotoxicity against human HeLa cells after 48 hrs by MTT assay
    		[PMID: 21185195]
    HFF IC50
    5584 nM
    Compound: AG-490
    Inhibition of fetal calf serum-induced proliferation of human foreskin fibroblast assessed as [3H]thymidine incorporation after 4 days by scintillation counting
    Inhibition of fetal calf serum-induced proliferation of human foreskin fibroblast assessed as [3H]thymidine incorporation after 4 days by scintillation counting
    		[PMID: 14593182]
    HT-29 IC50
    78.523 μM
    Compound: AG-490
    Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay
    Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay
    		[PMID: 21185195]
    Sf9 IC50
    > 10000 nM
    Compound: AG-490
    Inhibition of human recombinant GST-tagged JH1 domain (785 to1125) of JAK3 expressed in insect Sf9 cells by ELISA
    Inhibition of human recombinant GST-tagged JH1 domain (785 to1125) of JAK3 expressed in insect Sf9 cells by ELISA
    		[PMID: 14593182]
    T-cell IC50
    3750 nM
    Compound: AG-490
    Inhibition of IL2-induced proliferation of human T cells assessed as [3H]thymidine incorporation after 72 hrs by scintillation counting
    Inhibition of IL2-induced proliferation of human T cells assessed as [3H]thymidine incorporation after 72 hrs by scintillation counting
    		[PMID: 14593182]
    U-266 IC50
    > 12.5 μM
    Compound: AG-490
    Antitumor activity against human U266 cells after 24 to 72 hrs by MTT assay
    Antitumor activity against human U266 cells after 24 to 72 hrs by MTT assay
    		[PMID: 22036213]
    體外研究
    (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.
    體內(nèi)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 ?-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 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 (169.89 mM; 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)

    * "≥" means soluble, but saturation unknown.

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲(chǔ)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(chǔ)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(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?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請?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

      請依序添加每種溶劑： 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

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

      Solubility: 2.08 mg/mL (7.07 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.08 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

      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。
    動(dòng)物溶解方案計(jì)算器
    請輸入動(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)測溶解度，以下方案僅供參考，如有需要，請與 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，請謹(jǐn)慎選擇該方案。
    請確保第一步儲(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: 99.92%

    參考文獻(xiàn)
    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 ?-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.
    參考文獻(xiàn)

    完整儲(chǔ)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(chǔ)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(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?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請?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 3.3979 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.

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    Inquiry Information

    產(chǎn)品名稱：
    AG490
    目錄號(hào)：
    HY-12000
    需求量：