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.

Size Price Stock Quantity  
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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3 Customer Reviews

  • 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.

    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.

  • 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.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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.
Targets
EGFR [1]
(Cell-free assay)
HER2 [1]
(Cell-free assay)
PDGFR [1]
(Cell-free assay)
3 nM >100 μM >100 μM
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 NFr1fYZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYH+NVAxKM7:TR?= M4PVfWROW09? NYO4dXpvUUN3ME2zOE43KM7:TR?= NUPTbHQ2QDd3MkG0OS=>
U87MG.ΔEGFR MorZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlTLglExOCEQvF2= Ml;WSG1UVw>? M3jkPWlEPTB;OD63JO69VQ>? MoTtPFc2OjF2NR?=
U87MG.wtEGFR. MkmwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUL+NVAxKM7:TR?= NXPBU|RVTE2VTx?= M33ROGlEPTB;NEiuOEDPxE1? M{H6WVg4PTJzNEW=
U87MG MYrLbY5ie2ViYYPzZZk> M2rQNZ4yODBizszN NYX5e2J3TE2VTx?= NHLQZpVqdmirYnn0d{BGT0[UIIT5do9{cW6nIHvpcoF{\SCjY4Tpeol1gQ>? NFqwdFQ5PzV{MUS1
U87MG.ΔEGFR MXzLbY5ie2ViYYPzZZk> MVP+NVAxKM7:TR?= MX;EUXNQ NFO5bJNqdmirYnn0d{BGT0[UIIT5do9{cW6nIHvpcoF{\SCjY4Tpeol1gQ>? NITxRYI5PzV{MUS1
U87MG.wtEGFR. MnvqT4lv[XOnIHHzd4F6 MmDLglExOCEQvF2= NF;ycIZFVVOR M4iyS4lvcGmkaYTzJGVITlJidInyc5NqdmVia3nuZZNmKGGldHn2bZR6 MknoPFc2OjF2NR?=
HPV 16-immortalized human keratinocytes MoXqS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlLWglUxKM7:TR?= NWC2dWxnTE2VTx?= MYHpcohq[mm2czDj[YxtKGe{b4f0bC=> MnLEPVI5QDd6Mh?=
HPV 16-immortalized human keratinocytes Ml\2SpVv[3Srb36gZZN{[Xl? NWLsN2xLhjVyIN88US=> MYTEUXNQ NF\kS4FqdmS3Y3XzJIFzemW|dDDpckB1cGViQ3XscEBEgWOuZR?= M2rS[|kzQDh5OEK=
HPV 16-immortalized human keratinocytes NF7lfoJCeG:ydH;zbZMh[XO|YYm= NIHm[Ix,PTBizszN MYfEUXNQ MmrtbY5lfWOnczDhdI9xfG:|aYOu Ml;aPVI5QDd6Mh?=
A431 MWHLbY5ie2ViYYPzZZk> NEP5eZB,OTBizszN MmmzSG1UVw>? NIHmUohqdmirYnn0d{B1cGViYnHzZYwh[W6mIGTHSk3PuS2|dHnteYxifGWmIIT5do9{cW6nIIDoc5NxcG:{eXzheIlwdiCxZjD0bIUhTUeIUh?= NVXPfJhZOTB5MEKyOlI>
MDA-468  MmHUT4lv[XOnIHHzd4F6 NEXDPIF,OTBizszN M{Dj[2ROW09? M{HROYlvcGmkaYTzJJRp\SCkYYPhcEBidmRiVFfGMe6yNXO2aX31cIF1\WRidInyc5NqdmVicHjvd5Bpd3K7bHH0bY9vKG:oIITo[UBGT0[U M4TGclExPzB{Mk[y
A431 NIrBcmhHfW6ldHnvckBie3OjeR?= MYD+NVAh|ryP M{XxNGROW09? NW\sVGprcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> M{X5XFExPzB{Mk[y
MDA-MB-231 M1vrWGtqdmG|ZTDhd5NigQ>? MkTRglUh|ryP MnjjSG1UVw>? NXux[lFTcW6qaXLpeJMhTUeIIIP0bY12dGG2ZXSgdIhwe3Cqb4L5cIF1cW:wIH;mJGZMUFJ? M1XRdVEyODNyMUS2
CNE2 MmjtS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFzXd5kyODBizszN MXzEUXNQ NHjlNGpqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[nliOUiuOEU> MlS0NVE1OTB|MkK=
CNE2 Mom4T4lv[XOnIHHzd4F6 Ml7QglExOCEQvF2= M2rFSWROW09? MVPpcohq[mm2czDFS2ZTKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> MV:xNVQyODN{Mh?=
CNE2 M13TWGZ2dmO2aX;uJIF{e2G7 MmrKglExOCEQvF2= MX;EUXNQ M2XTSGlvcGmkaYTzJG1CWEtiYX7kJGFMXCCjY4TpeoF1cW:w M1rQdFEyPDFyM{Ky
CNE2 MWXGeY5kfGmxbjDhd5NigQ>? NEW3WWN,PTBizszN MV3EUXNQ MmnBZYZn\WO2czDj[YxtKGO7Y3zlJIRqe3S{aXL1eIlwdg>? NXTrbI5[OTF2MUCzNlI>
HSC-2 MWTLbY5ie2ViYYPzZZk> MWG4xsDPxE1? NIjBeJZFVVOR M{CzO4lvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBGT0[UIHHu[EBCc3R? MUGxO|Y5QTJ6NR?=
HSC-2 M{TU[WFxd3C2b4Ppd{Bie3OjeR?= M{jwbVjDqM7:TR?= NHHOVJdFVVOR NYexR25ncW6qaXLpeJMhTmG|LX3l[IlifGWmIHHwc5B1d3Orcx?= NEPNS|cyPzZ6OUK4OS=>
HEp-2 NYrTcHFPT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXn+NVAh|ryP M3TR[GROW09? Mnzw[Y5p[W6lZYOgc5Jq\G:waX6tbY5lfWOnZDDndo94fGhvaX7obYJqfG:{eR?= NIPjdnkzODJyMke0NS=>
SubG1 MYPBdI9xfG:|aYOgZZN{[Xl? MlPvglExKM7:TR?= MknvSG1UVw>? MXflcohidmOnczDvdolld26rbj3pcoR2[2WmIHHwc5B1d3Orcx?= NWfyOW1ZOjB{MEK3OFE>
HEp-2 NITnVHNHfW6ldHnvckBie3OjeR?= MoLqglExKM7:TR?= NG\WSphFVVOR MYjlcohidmOnczDPdolld26rbj3pcoR2[2WmIFLhfEBi[3SrdnH0bY9vNCCEY3ytNkBl\We{YXTheIlwdiCjbnSgV2lTXDFiaX7hZ5RqfmG2aX;u MXGyNFIxOjd2MR?=
H508 NIm4XpBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3LxfZ4yKM7:TR?= NWTPcJlqTE2VTx?= M3W0eI1qfGmpYYTld{BEWEZvbXXkbYF1\WRiSEWwPEBk\WyuIHfyc5d1cA>? NWT5V3Y5OjZ3MUS5NlQ>

... 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]

Protocol

Cell Research:

[2]

+ 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:

[4]

+ 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 <1 mg/mL
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 Information

Molecular Weight 315.75
Formula

C16H14ClN3O2

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