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)

Cat. No.: HY-13524 Purity: 99.22%
COA Handling Instructions

Molarity Calculator

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).

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

AG-1478 Chemical Structure

AG-1478 Chemical Structure

CAS No. : 153436-53-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 61 In-stock
Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Solid
1 mg USD 25 In-stock
5 mg USD 55 In-stock
10 mg USD 77 In-stock
50 mg USD 275 In-stock
100 mg USD 385 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 40 publication(s) in Google Scholar

Other Forms of AG-1478:

AG-1478 Related Antibodies

Top Publications Citing Use of Products

38 Publications Citing Use of MCE AG-1478

WB

    AG-1478 purchased from MedChemExpress. 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 MedChemExpress. 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.

    View All EGFR Isoform Specific Products:

    View All Isoforms
    EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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

     

    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].

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

    AG-1478 Related Antibodies
    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].

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

    315.75

    Formula

    C16H14ClN3O2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    COC1=CC2=NC=NC(NC3=CC=CC(Cl)=C3)=C2C=C1OC
    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 (158.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    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
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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 (6.59 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 (6.59 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 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  1% CMC/0.5% Tween-80 in Saline water

      Solubility: 5 mg/mL (15.84 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  1% CMC/0.5% Tween-80 in Saline water

      Solubility: 5 mg/mL (15.84 mM); Suspended solution; Need ultrasonic

    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: 99.22%

    COA (254 KB) LCMS (126 KB)

    Handling Instructions (2659 KB)
    References
    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.
    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 3.1671 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
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    AG-1478 Related Classifications

    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:

    AG-1478153436-53-4Tyrphostin AG-1478 NSC 693255AG1478AG 1478Tyrphostin AG1478Tyrphostin AG 1478NSC693255NSC 693255NSC-693255EGFRHCVInfluenza VirusEpidermal growth factor receptorErbB-1HER1Hepatitis C virusantiviralencephalomyocarditisvirusEMCVobesitymyocardialinjurycardiovasculardiseasescancerchemotherapyInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Salutation

    Applicant Name *

    		 

    Email Address *

    Phone Number *

    		 

    Organization Name *

    Department *

    		 

    Requested quantity *

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    AG-1478
    Cat. No.:
    HY-13524
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.