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
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USD 110 In stock
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Cited by 24 Publications

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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)
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 MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYr2b2ZbhjFyMDFOwG0> NWnTe|ZuTE2VTx?= NUDFPHlrUUN3ME2zOE43KM7:TR?= MWe4O|UzOTR3
U87MG.ΔEGFR Ml3aS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlXrglExOCEQvF2= NYDWNG5NTE2VTx?= MULJR|UxRThwNzFOwG0> M{SwbFg4PTJzNEW=
U87MG.wtEGFR. MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYTuZYJ7hjFyMDFOwG0> MUjEUXNQ NETQe5VKSzVyPUS4MlQh|ryP M1TVUlg4PTJzNEW=
U87MG MmrCT4lv[XOnIHHzd4F6 NUTMbGduhjFyMDFOwG0> M1vkN2ROW09? M3i4WYlvcGmkaYTzJGVITlJidInyc5NqdmVia3nuZZNmKGGldHn2bZR6 M4HwSlg4PTJzNEW=
U87MG.ΔEGFR MojHT4lv[XOnIHHzd4F6 NUjlTWFqhjFyMDFOwG0> NIrVdmtFVVOR NGmwO4pqdmirYnn0d{BGT0[UIIT5do9{cW6nIHvpcoF{\SCjY4Tpeol1gQ>? NYHXTZBlQDd3MkG0OS=>
U87MG.wtEGFR. M3n0VmtqdmG|ZTDhd5NigQ>? Mn3BglExOCEQvF2= NH\CdoZFVVOR MnuxbY5pcWKrdIOgSWdHWiC2eYLvd4lv\SCtaX7hd4Uh[WO2aY\peJk> MYm4O|UzOTR3
HPV 16-immortalized human keratinocytes NV7qbW9VT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NH\3b4N,PTBizszN NXSxNmIzTE2VTx?= MVTpcohq[mm2czDj[YxtKGe{b4f0bC=> MY[5Nlg5Pzh{
HPV 16-immortalized human keratinocytes MoHKSpVv[3Srb36gZZN{[Xl? MWH+OVAh|ryP NFzibY9FVVOR M{jteolv\HWlZYOgZZJz\XO2IHnuJJRp\SCFZXzsJGN6[2yn NFrF[lM6Ojh6N{iy
HPV 16-immortalized human keratinocytes Mnf3RZBweHSxc3nzJIF{e2G7 NEe0T2p,PTBizszN NGHVVZpFVVOR MV\pcoR2[2W|IHHwc5B1d3Orcz6= MWi5Nlg5Pzh{
A431 MXvLbY5ie2ViYYPzZZk> NF7UOJh,OTBizszN M{PMeGROW09? Mlm0bY5pcWKrdIOgeIhmKGKjc3HsJIFv\CCWR1[t{tEue3SrbYXsZZRm\CC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44hd2ZidHjlJGVITlJ? NUHkTpprOTB5MEKyOlI>
MDA-468  M2TDOWtqdmG|ZTDhd5NigQ>? MlGzglExKM7:TR?= NGrTTWpFVVOR NYLlbm9RcW6qaXLpeJMhfGinIHLhd4FtKGGwZDDUS2Yu|rFvc4TpcZVt[XSnZDD0fZJwe2mwZTDwbI9{eGixconsZZRqd25ib3[geIhmKEWJRmK= NVO1cYRxOTB5MEKyOlI>
A431 M1;z[mZ2dmO2aX;uJIF{e2G7 NXfKXVUzhjFyIN88US=> MoTkSG1UVw>? M1PaNolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NGHsb4wyODdyMkK2Ni=>
MDA-MB-231 Mn7OT4lv[XOnIHHzd4F6 MXP+OUDPxE1? NWTUc5hKTE2VTx?= MWDpcohq[mm2czDFS2Yhe3SrbYXsZZRm\CCyaH;zdIhwenmuYYTpc44hd2ZiRlvIVi=> M1juUlEyODNyMUS2
CNE2 NUnQcFdpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4T3ZVExOCEQvF2= NX\jS3Z[TE2VTx?= NYLBfGxHcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGK7IEm4MlQm M{HHS|EyPDFyM{Ky
CNE2 NFe4U5NMcW6jc3WgZZN{[Xl? NHrHd4x,OTByIN88US=> NG\rRYpFVVOR MlfBbY5pcWKrdIOgSWdHWiC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> NUnsW3pWOTF2MUCzNlI>
CNE2 M2H6W2Z2dmO2aX;uJIF{e2G7 MmXQglExOCEQvF2= M1XlSmROW09? M4fxZ2lvcGmkaYTzJG1CWEtiYX7kJGFMXCCjY4TpeoF1cW:w MYGxNVQyODN{Mh?=
CNE2 MmfmSpVv[3Srb36gZZN{[Xl? MknTglUxKM7:TR?= NF;WbodFVVOR NWDhfoR{[W[oZXP0d{Bk\WyuIHP5Z4xmKGSrc4TybYJ2fGmxbh?= NIjySm4yOTRzMEOyNi=>
HSC-2 NHfrNXhMcW6jc3WgZZN{[Xl? MV24xsDPxE1? M13pVmROW09? NYmwOoRIcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEWJRmKgZY5lKEGtdB?= NVLjfpVrOTd4OEmyPFU>
HSC-2 NV;PUW8ySXCxcITvd4l{KGG|c3H5 MluwPOKh|ryP MVvEUXNQ NUPFTVRHcW6qaXLpeJMhTmG|LX3l[IlifGWmIHHwc5B1d3Orcx?= NF\XdWYyPzZ6OUK4OS=>
HEp-2 M2\WdGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFyxOYR,OTBizszN MYTEUXNQ M{[zU4VvcGGwY3XzJI9zcWSxbnnuMYlv\HWlZXSg[5Jwf3SqLXnubIljcXSxcom= MVqyNFIxOjd2MR?=
SubG1 M4rBemFxd3C2b4Ppd{Bie3OjeR?= NXPpOGVohjFyIN88US=> MXnEUXNQ NGHUfY9mdmijbnPld{Bwemmmb37pck1qdmS3Y3XkJIFxd3C2b4Ppdy=> NIHvPGMzODJyMke0NS=>
HEp-2 NF;vb4RHfW6ldHnvckBie3OjeR?= NX;C[5NJhjFyIN88US=> NGqwRnhFVVOR MVvlcohidmOnczDPdolld26rbj3pcoR2[2WmIFLhfEBi[3SrdnH0bY9vNCCEY3ytNkBl\We{YXTheIlwdiCjbnSgV2lTXDFiaX7hZ5RqfmG2aX;u M4q1N|IxOjB{N{Sx
H508 MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2Dlbp4yKM7:TR?= MXfEUXNQ NH3Ib|lucXSrZ3H0[ZMhS1CILX3l[IlifGWmIFi1NFgh[2WubDDndo94fGh? MXeyOlUyPDl{NB?=

... 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 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID