AG-1478 (Tyrphostin AG-1478)

Catalog No.S2728 Synonyms: NSC 693255

AG-1478 (Tyrphostin AG-1478) Chemical Structure

Molecular Weight(MW): 315.75

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

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In DMSO USD 64 In stock
USD 70 In stock
USD 110 In stock
USD 220 In stock
USD 370 In stock
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Cited by 9 Publications

3 Customer Reviews

  • A549 cells were treated with G15 (a specific antagonist of GPR30, 1 uM), AG1478 (a potent antagonist of EGFR, 10 uM), BPA (10-5 M) alone for 15 min or BPA after a 90-min pretreatment with G15 or AG1478 for 15 min. Then the expression of p-ERK1/2 and total ERK1/2 were measured by western blot analysis.

    Biomed Pharmacother 2014 10.1016/j.biopha.2014.09.003. AG-1478 (Tyrphostin AG-1478) purchased from Selleck.

    The inhibition of tyrosine kinase activity of EGFR abolished a morphological change associated with EMT (A) and EGF-mediated TACC3 induction (B). Cells were treated with EGF or EGF+AG1478 for 24 h and then subjected to western blot analysis. β-actin was used as a loading control.The intensity of bands was quantified using imageJ software and normalized to β-actin.

    PLoS One, 2013, 8(8): e70353. AG-1478 (Tyrphostin AG-1478) purchased from Selleck.

  • BPA 1 nM, G-1 (a specific agonist of GPR30) alone (10 nM) or after a 90-min pretreatment with G15 (a specific antagonist of GPR30, 1 uM), PD 98059 (an ERK1/2 antagonist, 10 uM), AG-1478 (a potent antagonist of EGFR, 10 uM), or the mixture (G15, PD 98059, and AG-1478). ERK1/2 phosphorylation in TM4 cells exposure to different compounds with the concentrations mentioned above for 15 min. Values shown are expressed in the percentage of control (steroid-free medium) given as the mean ?SD of three independent experiments (n = 3). *p < 0.05 compared with control; **p < 0.01 compared with control.

    Toxicol Lett 2014 226(1), 81-9. AG-1478 (Tyrphostin AG-1478) purchased from Selleck.

Purity & Quality Control

Choose Selective EGFR Inhibitors

Biological Activity

Description AG-1478 (Tyrphostin AG-1478) is a selective EGFR inhibitor with IC50 of 3 nM in cell-free assays, almost no activity on HER2-Neu, PDGFR, Trk, Bcr-Abl and InsR.
EGFR [1]
(Cell-free assay)
3 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U87MG.wtEGFR. MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoS0glExOCEQvF2= NYHnOW1oTE2VTx?= M3XIOGlEPTB;NEiuOEDPxE1? M3PMblg4PTJzNEW=
U87MG MV3LbY5ie2ViYYPzZZk> NFHBXI1,OTByIN88US=> M17U[WROW09? MlzZbY5pcWKrdIOgSWdHWiC2eYLvd4lv\SCtaX7hd4Uh[WO2aY\peJk> M2P4flg4PTJzNEW=
U87MG.ΔEGFR MmmyT4lv[XOnIHHzd4F6 NWnrTGc{hjFyMDFOwG0> MV3EUXNQ NGXrV3pqdmirYnn0d{BGT0[UIIT5do9{cW6nIHvpcoF{\SCjY4Tpeol1gQ>? NGDyWG85PzV{MUS1
U87MG.wtEGFR. MmD5T4lv[XOnIHHzd4F6 M3\5R54yODBizszN NFzDPIVFVVOR Mlv4bY5pcWKrdIOgSWdHWiC2eYLvd4lv\SCtaX7hd4Uh[WO2aY\peJk> MYm4O|UzOTR3
HPV 16-immortalized human keratinocytes NWHyZW9nT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mk\VglUxKM7:TR?= NYXqe3dkTE2VTx?= NIHzVndqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M4[yblkzQDh5OEK=
HPV 16-immortalized human keratinocytes NEnrRlRHfW6ldHnvckBie3OjeR?= MUP+OVAh|ryP NYPrWWRpTE2VTx?= MkTHbY5lfWOnczDhdpJme3RiaX6geIhmKEOnbHygR5lkdGV? NI\GVGI6Ojh6N{iy
HPV 16-immortalized human keratinocytes NELPN3NCeG:ydH;zbZMh[XO|YYm= NWTJWJBlhjVyIN88US=> Ml31SG1UVw>? Ml[1bY5lfWOnczDhdI9xfG:|aYOu NYTIVGd6QTJ6OEe4Ni=>
A431 NFPN[49McW6jc3WgZZN{[Xl? NFyxUnR,OTBizszN NVS5V3N5TE2VTx?= M3LVcIlvcGmkaYTzJJRp\SCkYYPhcEBidmRiVFfGMe6yNXO2aX31cIF1\WRidInyc5NqdmVicHjvd5Bpd3K7bHH0bY9vKG:oIITo[UBGT0[U NFzWOpcyODdyMkK2Ni=>
MDA-468  NEfTcIxMcW6jc3WgZZN{[Xl? MmDLglExKM7:TR?= MYnEUXNQ M{PrWYlvcGmkaYTzJJRp\SCkYYPhcEBidmRiVFfGMe6yNXO2aX31cIF1\WRidInyc5NqdmVicHjvd5Bpd3K7bHH0bY9vKG:oIITo[UBGT0[U M3Tm[FExPzB{Mk[y
A431 NIrqZVZHfW6ldHnvckBie3OjeR?= NYL0RYlwhjFyIN88US=> M2XQ[WROW09? M4HZfolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= M13ZZlExPzB{Mk[y
CNE2 M{\HPWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M374OlExOCEQvF2= NYnacVNmTE2VTx?= NHfLXpFqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[nliOUiuOEU> NYXzS4lbOTF2MUCzNlI>
CNE2 NHK5NZJMcW6jc3WgZZN{[Xl? NY\PNWl5hjFyMDFOwG0> MlfpSG1UVw>? NInOVoJqdmirYnn0d{BGT0[UIIT5do9{cW6nIIDoc5NxcG:{eXzheIlwdg>? NGXnVmUyOTRzMEOyNi=>
CNE2 MmXJSpVv[3Srb36gZZN{[Xl? M3XKfZ4yODBizszN MkHGSG1UVw>? NUj2UXlIUW6qaXLpeJMhVUGSSzDhcoQhSUuWIHHjeIl3[XSrb36= M{jjVVEyPDFyM{Ky
CNE2 NITmSnBHfW6ldHnvckBie3OjeR?= NGHyPZl,PTBizszN M3;XbmROW09? MYXh[oZm[3S|IHPlcIwh[3mlbHWg[Il{fHKrYoX0bY9v NUS4XGo1OTF2MUCzNlI>
HSC-2 MXLLbY5ie2ViYYPzZZk> MWm4xsDPxE1? NILlcZlFVVOR NVfU[VFQcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEWJRmKgZY5lKEGtdB?= NWnId245OTd4OEmyPFU>
HSC-2 Ml22RZBweHSxc3nzJIF{e2G7 MYO4xsDPxE1? MWHEUXNQ M1nwWYlvcGmkaYTzJGZiey2vZXTpZZRm\CCjcH;weI9{cXN? NUHPeIxzOTd4OEmyPFU>
HEp-2 M4PWe2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Ml3aglExKM7:TR?= MorsSG1UVw>? Mlz4[Y5p[W6lZYOgc5Jq\G:waX6tbY5lfWOnZDDndo94fGhvaX7obYJqfG:{eR?= M3XTZVIxOjB{N{Sx
SubG1 NXzIeIhSSXCxcITvd4l{KGG|c3H5 MV3+NVAh|ryP MnPrSG1UVw>? NWG3foR2\W6qYX7j[ZMhd3KrZH;ubY4ucW6mdXPl[EBieG:ydH;zbZM> NX\VbmpROjB{MEK3OFE>
HEp-2 NEO3RWxHfW6ldHnvckBie3OjeR?= MkTqglExKM7:TR?= M2H1e2ROW09? MUnlcohidmOnczDPdolld26rbj3pcoR2[2WmIFLhfEBi[3SrdnH0bY9vNCCEY3ytNkBl\We{YXTheIlwdiCjbnSgV2lTXDFiaX7hZ5RqfmG2aX;u MVWyNFIxOjd2MR?=
H508 NE\IUlNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NULMTpFFhjFizszN MlztSG1UVw>? MUTtbZRq\2G2ZYOgR3BHNW2nZHnheIVlKEh3MEigZ4VtdCCpcn;3eIg> M4niZ|I3PTF2OUK0

... Click to View More Cell Line Experimental Data

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]


Cell Research:


+ Expand
  • 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.

    (Only for Reference)
Animal Research:


+ Expand
  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 25 mg/mL (79.17 mM)
Ethanol 13 mg/mL (41.17 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
15% Captisol
For best results, use promptly after mixing.
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.

Chemical Information

Molecular Weight 315.75


CAS No. 153436-53-4
Storage powder
in solvent
Synonyms NSC 693255

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID