AG-1478 (Tyrphostin AG-1478)

For research use only.

Catalog No.S2728 Synonyms: NSC 693255

63 publications

AG-1478 (Tyrphostin AG-1478) Chemical Structure

CAS No. 153436-53-4

AG-1478 (Tyrphostin AG-1478, NSC 693255) 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. AG-1478 (Tyrphostin AG-1478) inhibits encephalomyocarditis virus (EMCV) and hepatitis c virus (HCV) by targeting phosphatidylinositol 4-kinase IIIα (PI4KA).

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Selleck's AG-1478 (Tyrphostin AG-1478) has been cited by 63 publications

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Biological Activity

Description AG-1478 (Tyrphostin AG-1478, NSC 693255) 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. AG-1478 (Tyrphostin AG-1478) inhibits encephalomyocarditis virus (EMCV) and hepatitis c virus (HCV) by targeting phosphatidylinositol 4-kinase IIIα (PI4KA).
Targets
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 NWrMeWJ4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MV\+NVAxKM7:TR?= MnnJSG1UVw>? MV;JR|UxRTN2Lk[g{txO MmjRPFc2OjF2NR?=
U87MG.ΔEGFR NHm5fHZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWP+NVAxKM7:TR?= NWTDRpVLTE2VTx?= NYLkTlE2UUN3ME24Mlch|ryP MX:4O|UzOTR3
U87MG.wtEGFR. NYe2cZFPT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEn0VIZ,OTByIN88US=> NXfTNVFSTE2VTx?= MXHJR|UxRTR6LkSg{txO M2PBTFg4PTJzNEW=
U87MG NV3sWYZzU2mwYYPlJIF{e2G7 M4HRVZ4yODBizszN NGi2XpVFVVOR NFixbY9qdmirYnn0d{BGT0[UIIT5do9{cW6nIHvpcoF{\SCjY4Tpeol1gQ>? M{L5[lg4PTJzNEW=
U87MG.ΔEGFR MnvxT4lv[XOnIHHzd4F6 MXz+NVAxKM7:TR?= NYDvOIs6TE2VTx?= NHLkNoJqdmirYnn0d{BGT0[UIIT5do9{cW6nIHvpcoF{\SCjY4Tpeol1gQ>? MX[4O|UzOTR3
U87MG.wtEGFR. NIfxRnhMcW6jc3WgZZN{[Xl? NXXFVWVrhjFyMDFOwG0> M17UO2ROW09? NYXIbJF2cW6qaXLpeJMhTUeIUjD0fZJwe2mwZTDrbY5ie2ViYXP0bZZqfHl? NGPFSmY5PzV{MUS1
HPV 16-immortalized human keratinocytes NX2zelByT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MX;+OVAh|ryP NX7SbVdsTE2VTx?= MlnibY5pcWKrdIOgZ4VtdCCpcn;3eIg> M1HqU|kzQDh5OEK=
HPV 16-immortalized human keratinocytes NH\wSodHfW6ldHnvckBie3OjeR?= MX\+OVAh|ryP Ml\CSG1UVw>? NXTO[3BWcW6mdXPld{BienKnc4SgbY4hfGinIFPlcIwhS3mlbHW= Mn24PVI5QDd6Mh?=
HPV 16-immortalized human keratinocytes NEO3c|VCeG:ydH;zbZMh[XO|YYm= NGrsfnJ,PTBizszN Ml\RSG1UVw>? M4fXV4lv\HWlZYOgZZBweHSxc3nzMi=> M4jKTlkzQDh5OEK=
A431 M1L0bmtqdmG|ZTDhd5NigQ>? MmflglExKM7:TR?= MkfZSG1UVw>? MVrpcohq[mm2czD0bIUh[mG|YXygZY5lKFSJRj5OtU1{fGmvdXzheIVlKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvckBw\iC2aHWgSWdHWg>? NG\ncZIyODdyMkK2Ni=>
MDA-468  NHzadohMcW6jc3WgZZN{[Xl? NIjROpN,OTBizszN NXm5VlhyTE2VTx?= NFjJdJJqdmirYnn0d{B1cGViYnHzZYwh[W6mIGTHSk3PuS2|dHnteYxifGWmIIT5do9{cW6nIIDoc5NxcG:{eXzheIlwdiCxZjD0bIUhTUeIUh?= Mn\JNVA4ODJ{NkK=
A431 M4i2TGZ2dmO2aX;uJIF{e2G7 MVP+NVAh|ryP NX:0cnhjTE2VTx?= M1:3cIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= Mn:2NVA4ODJ{NkK=
MDA-MB-231 M{T4SGtqdmG|ZTDhd5NigQ>? MYj+OUDPxE1? MXnEUXNQ NF2xPYVqdmirYnn0d{BGT0Zic4TpcZVt[XSnZDDwbI9{eGixconsZZRqd25ib3[gSmtJWg>? NWDpN|loOTFyM{CxOFY>
CNE2 MnHyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmnvNVAxKM7:TR?= NHjE[ndFVVOR NVzF[3dGcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGK7IEm4MlQm MkjSNVE1OTB|MkK=
CNE2 NYjaVIllU2mwYYPlJIF{e2G7 MmnLglExOCEQvF2= M{TQdGROW09? M2fXOIlvcGmkaYTzJGVITlJidInyc5NqdmVicHjvd5Bpd3K7bHH0bY9v M4HlelEyPDFyM{Ky
CNE2 M33EVWZ2dmO2aX;uJIF{e2G7 MXT+NVAxKM7:TR?= M1zOVGROW09? NX7FfJgzUW6qaXLpeJMhVUGSSzDhcoQhSUuWIHHjeIl3[XSrb36= NFH3UlMyOTRzMEOyNi=>
CNE2 M{HUNmZ2dmO2aX;uJIF{e2G7 M{T0S542OCEQvF2= NXSwdoNrTE2VTx?= Mn76ZYZn\WO2czDj[YxtKGO7Y3zlJIRqe3S{aXL1eIlwdg>? MmflNVE1OTB|MkK=
HSC-2 NWL5VJdpU2mwYYPlJIF{e2G7 MWm4xsDPxE1? Moj6SG1UVw>? NWPpZXlLcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEWJRmKgZY5lKEGtdB?= MlvoNVc3QDl{OEW=
HSC-2 NYrte4pMSXCxcITvd4l{KGG|c3H5 M{PzXVjDqM7:TR?= MkPSSG1UVw>? MY\pcohq[mm2czDGZZMudWWmaXH0[YQh[XCxcITvd4l{ MYOxO|Y5QTJ6NR?=
HEp-2 MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVz+NVAh|ryP MljZSG1UVw>? MVHlcohidmOnczDvdolld26rbj3pcoR2[2WmIHfyc5d1cC2rbnjpZol1d3K7 NVr3R2dJOjB{MEK3OFE>
SubG1 NFjTdnhCeG:ydH;zbZMh[XO|YYm= NFzxTZp,OTBizszN Mnz5SG1UVw>? NUL0T|Y5\W6qYX7j[ZMhd3KrZH;ubY4ucW6mdXPl[EBieG:ydH;zbZM> NHz1RpQzODJyMke0NS=>
HEp-2 NIPySJRHfW6ldHnvckBie3OjeR?= MX7+NVAh|ryP MX3EUXNQ MUPlcohidmOnczDPdolld26rbj3pcoR2[2WmIFLhfEBi[3SrdnH0bY9vNCCEY3ytNkBl\We{YXTheIlwdiCjbnSgV2lTXDFiaX7hZ5RqfmG2aX;u NWHiflFDOjB{MEK3OFE>
H508 NV\1O5dXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmqzglEh|ryP NXiydIp7TE2VTx?= M3nGWo1qfGmpYYTld{BEWEZvbXXkbYF1\WRiSEWwPEBk\WyuIHfyc5d1cA>? MkS2NlY2OTR7MkS=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
EGFR / Neu / p-Tyr ; 

PubMed: 10931950     


MCF-10AyTE cells with or without AG-1478. After 24 h, cell lysates were prepared in EBC buffer and subjected to immunoblot procedures for EGFR, ErbB-2yNeu, and P-Tyr. Levels of a 180-kDa P-Tyr band, probably representing EGFR and ErbB-2yNeu, were reduced by AG-1478 without any change in receptor protein content.

Shc / PLC-γ1 ; 

PubMed: 10931950     


MCF-10AyTE cells with or without AG-1478. After 24 h, cell lysates were prepared in EBC buffer and subjected to immunoblot procedures for EGFR, ErbB-2yNeu, and P-Tyr. Levels of a 180-kDa P-Tyr band, probably representing EGFR and ErbB-2yNeu, were reduced by AG-1478 without any change in receptor protein content.

10931950
Growth inhibition assay
Cell viability ; 

PubMed: 25258648     


Dose-dependent effects of EGFR inhibitor AG-1478 on EGF-induced cell viability in OVCAR-3 cells. Cells were treated for 48 h with EGF (10 ng/mL) alone or in combination of AG-1478 (0, 0.25, 0.5 and 1 µmol/L). A cell viability assay was performed using MTT and values were normalized to untreated controls (no EGF, no inhibitors). Blackened bars were EGF treated. *, ** indicate a significant increase (p≤0.05) and # indicates a significant decrease (p≤0.05) between groups by ANOVA and Tukey’s pairwise comparisons. Experiments were performed in triplicate and all data are shown as mean ± SEM.

25258648
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]

Protocol

Cell Research:

[2]

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  • 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:

[4]

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  • Animal Models: Female BALB/c nu/nu mice inoculated s.c. with A431 or U87MG.Δ2-7 tumor cells
  • 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
Formula

C16H14ClN3O2

CAS No. 153436-53-4
Storage powder
in solvent
Synonyms NSC 693255
Smiles COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=CC=C3)Cl)OC

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID