AG-1478 (Tyrphostin AG-1478)

AG-1478 (Tyrphostin AG-1478) is a selective EGFR inhibitor with IC50 of 3 nM, almost no activity on HER2-Neu, PDGFR, Trk, Bcr-Abl and InsR.

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AG-1478 (Tyrphostin AG-1478) Chemical Structure

AG-1478 (Tyrphostin AG-1478) Chemical Structure
Molecular Weight: 315.75

Validation & Quality Control

Customer Reviews(2)

Quality Control & MSDS

Related Compound Libraries

AG-1478 (Tyrphostin AG-1478) is available in the following compound libraries:

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  • FDA-approved Inhibitor

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  • Newest EGFR Inhibitor

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Product Information

  • Inhibition Profile
  • Compare EGFR Inhibitors
    Compare EGFR Products
  • Research Area
  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

Description AG-1478 (Tyrphostin AG-1478) is a selective EGFR inhibitor with IC50 of 3 nM, almost no activity on HER2-Neu, PDGFR, Trk, Bcr-Abl and InsR.
Targets EGFR HER2 PDGFR
IC50 3 nM [1] >100 μM [1] >100 μM [1]
In vitro AG-1478 is high selective over ErbB2 and PDGFR with IC50 of >100 μM. [1] AG-1478 preferentially inhibits U87MG cells expressing truncated EGFR with IC50 of 8.7 μM, compared to those expressing endogenous wt EGFR or overexpressing exogenous wt EGFR with IC50 of 34.6 μM and 48.4 μM, respectively, and inhibits the DNA synthesis with IC50 of 4.6 μM, 19.67 μM, and 35.2 μM, respectively. AG-1478 also preferentially inhibits the tyrosine kinase activity and autophosphorylation of the ΔEGFR compared to endogenous or overexpressed exogenous wt EGFR. [2] AG-1478 (0.25 μM) abolishes the MAPK activation induced by Ang II, a Ca2+ ionophore as well as EGF but not by a phorbol ester or platelet-derived growth factor-BB in the VSMC. [3] AG-1478 inhibits EGF-induced mitogenesis of the BaF/ERX and LIM1215 cells with IC50 of 0.07 μM and 0.2 μM, respectively. [6] AG1478 is able to inhibit the function of ATP-binding cassette (ABC) transporters such as ABCB1 and ABCG2, with a more pronounced effect on ABCG2. [7]
In vivo Administration of AG-1478 blocks phosphorylation of the EGFR at the tumor site and inhibits the growth of A431 xenografts that overexpress the WT EGFR and glioma xenografts expressing the de2-7 EGFR. Even subtherapeutic doses of AG-1478 significantly enhance the efficacy of cytotoxic drugs, with the combination of AG-1478 and temozolomide displaying synergistic antitumor activity against human glioma xenografts. The combination of AG-1478 and an anti-EGFR antibody (mAb 806) displays additive and in some cases synergistic, antitumor activity against tumor xenografts overexpressing the EGFR. [4] The combination of AG-1478 (0.4 mg) with a single dose of 25 μCi 90Y-CHX-A''-DTPA-hu3S193 results in a significant enhancement of efficacy compared with either agent alone. [5]
Features

Protocol(Only for Reference)

Cell Assay:

[2]

Cell lines U87MG
Concentrations Dissolved in DMSO, final concentrations ~100 μM
Incubation Time 72 hours
Method

Cells are exposed to different concentrations of AG-1478 for 72 hours in 96-well plates. The effects of AG-1478 on cell growth are examined using an Alamar Blue assay. A 20-μL aliquot of Alamar Blue is added to each well, and its absorbance is determined using a Spectromax Scanning Micro plate Reader. The effects of AG-1478 are expressed as percentage of growth inhibition using untreated cells as the control (0% inhibition). Cellular DNA synthesis is determined using a [3H]thymidine incorporation assay.

Animal Study:

[4]

Animal Models Female BALB/c nu/nu mice inoculated s.c. with A431 or U87MG.Δ2-7 tumor cells
Formulation Dissolved in 100 mM Captisol
Dosages ~1 mg/kg
Administration Injection i.p. three times per week
Solubility 15% Captisol, 30 mg/mL
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
1

References

Chemical Information

Download AG-1478 (Tyrphostin AG-1478) SDF
Molecular Weight (MW) 315.75
Formula

C16H14ClN3O2

CAS No. 153436-53-4
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms NSC 693255
Solubility (25°C) * In vitro DMSO 25 mg/mL (79 mM)
Water <1 mg/mL (<1 mM)
Ethanol 13 mg/mL (41 mM)
In vivo 15% Captisol, 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name N-(3-chlorophenyl)-6,7-dimethoxyquinazolin-4-amine

Research Area

Customer Reviews (2)


Click to enlarge
Rating
Source PLoS One. 2013 Aug 1;8(8):e70353 . AG-1478 (Tyrphostin AG-1478) purchased from Selleck
Method Western blot
Cell Lines EGFR-expressing cells
Concentrations 5 uM
Incubation Time 24 h
Results Treatment with 5 μM of AG1478 abolished EGF-induced morphological changes and TACC3 induction , and as a consequence, EGF-mediated EMT was inhibited.

Click to enlarge
Rating
Source PLoS One. 2013 Aug 1;8(8):e70353 . AG-1478 (Tyrphostin AG-1478) purchased from Selleck
Method microscope imaging
Cell Lines EGFR-expressing cells
Concentrations 5 uM
Incubation Time 24 h
Results Treatment with 5 μM of AG1478 abolished EGF-induced morphological changes and TACC3 induction.

Product Citations (5)

Tech Support & FAQs

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