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

AG490  (Synonyms: Tyrphostin AG490; Tyrphostin B42)

Cat. No.: HY-12000 Purity: 99.97%
COA Handling Instructions

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

For research use only. We do not sell to patients.

AG490 Chemical Structure

AG490 Chemical Structure

CAS No. : 133550-30-8

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Solid + Solvent
10 mM * 1 mL in DMSO
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USD 61 In-stock
Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Solid
5 mg USD 35 In-stock
10 mg USD 55 In-stock
50 mg USD 98 In-stock
100 mg USD 127 In-stock
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Customer Review

Based on 108 publication(s) in Google Scholar

Other Forms of AG490:

Top Publications Citing Use of Products

97 Publications Citing Use of MCE AG490

IF
WB

    AG490 purchased from MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target[1]

    EGFR

     

    Stat-3

     

    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].

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

    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].

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

    Molecular Weight

    294.30

    Formula

    C17H14N2O3

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(NCC1=CC=CC=C1)/C(C#N)=C/C2=CC=C(O)C(O)=C2

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (169.89 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (7.07 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (7.07 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.97%

    References
    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.

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 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
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      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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