AG-1478 (Tyrphostin AG-1478) 化学構造
分子量: 315.75





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  • 研究分野
  • Combination Therapy



製品説明 AG-1478(Tyrphostin AG-1478)は、3nMのIC50による選択的な上皮細胞増殖因子受容体(EGFR)チロシン・キナーゼ阻害剤です。



3 nM [1]

In vitro試験 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
U87MG MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmryglExOCEQvF2= NXPPcVdOTE2VTx?= M2TlN2lEPTB;M{SuOkDPxE1? NIXENpY5PzV{MUS1
U87MG.ΔEGFR MULHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2fkOp4yODBizszN MmTTSG1UVw>? NX\XOZVzUUN3ME24Mlch|ryP MVi4O|UzOTR3
U87MG.wtEGFR. NEXKc2xIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkfYglExOCEQvF2= M4nScGROW09? MWnJR|UxRTR6LkSg{txO M{fKVFg4PTJzNEW=
U87MG MnGzT4lv[XOnIHHzd4F6 NXPQZ|dThjFyMDFOwG0> M3jMOGROW09? NIPscINqdmirYnn0d{BGT0[UIIT5do9{cW6nIHvpcoF{\SCjY4Tpeol1gQ>? M3v3TFg4PTJzNEW=
U87MG.ΔEGFR M4qxb2tqdmG|ZTDhd5NigQ>? MUD+NVAxKM7:TR?= Mnj6SG1UVw>? MV;pcohq[mm2czDFS2ZTKHS7cn;zbY5mKGurbnHz[UBi[3Srdnn0fS=> NE\5e2I5PzV{MUS1
U87MG.wtEGFR. MWfLbY5ie2ViYYPzZZk> NHz2UoN,OTByIN88US=> M{X4fWROW09? NXm3XHBIcW6qaXLpeJMhTUeIUjD0fZJwe2mwZTDrbY5ie2ViYXP0bZZqfHl? MWW4O|UzOTR3
HPV 16-immortalized human keratinocytes M{TXcWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3TofJ42OCEQvF2= M2jKUWROW09? MYXpcohq[mm2czDj[YxtKGe{b4f0bC=> M1Xzd|kzQDh5OEK=
HPV 16-immortalized human keratinocytes MXrGeY5kfGmxbjDhd5NigQ>? MUT+OVAh|ryP M3LXcmROW09? NF[wV3NqdmS3Y3XzJIFzemW|dDDpckB1cGViQ3XscEBEgWOuZR?= NFzhSZc6Ojh6N{iy
HPV 16-immortalized human keratinocytes MkX0RZBweHSxc3nzJIF{e2G7 M{m3eJ42OCEQvF2= NVX0RYNGTE2VTx?= MmOzbY5lfWOnczDhdI9xfG:|aYOu NFK3T|I6Ojh6N{iy
A431 Mnz0T4lv[XOnIHHzd4F6 NXHQb2c2hjFyIN88US=> NGjyNJFFVVOR MnHybY5pcWKrdIOgeIhmKGKjc3HsJIFv\CCWR1[t{tEue3SrbYXsZZRm\CC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44hd2ZidHjlJGVITlJ? M1vzbVExPzB{Mk[y
MDA-468  MUXLbY5ie2ViYYPzZZk> Ml;rglExKM7:TR?= MVrEUXNQ M1TMeYlvcGmkaYTzJJRp\SCkYYPhcEBidmRiVFfGMe6yNXO2aX31cIF1\WRidInyc5NqdmVicHjvd5Bpd3K7bHH0bY9vKG:oIITo[UBGT0[U M4TTXlExPzB{Mk[y
MDA-MB-231 Ml2yT4lv[XOnIHHzd4F6 M3P2Op42KM7:TR?= NIe4[JZFVVOR M{O3TYlvcGmkaYTzJGVITiC|dHnteYxifGWmIIDoc5NxcG:{eXzheIlwdiCxZjDGT2hT MmjqNVExOzBzNE[=
CNE2 NGPVRVNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXGxNFAh|ryP M4\i[GROW09? NV7j[IpOcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGK7IEm4MlQm NXH0UWozOTF2MUCzNlI>
CNE2 NH3TNoVMcW6jc3WgZZN{[Xl? NGi3PWR,OTByIN88US=> MWPEUXNQ MXjpcohq[mm2czDFS2ZTKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> M2O5PVEyPDFyM{Ky
CNE2 Mn;USpVv[3Srb36gZZN{[Xl? MoKyglUxKM7:TR?= MnXoSG1UVw>? NIDGZWNi\m[nY4TzJINmdGxiY4njcIUh\Gm|dILpZpV1cW:w MmS0NVE1OTB|MkK=
HSC-2 M3juXWtqdmG|ZTDhd5NigQ>? NGDOW5A5yqEQvF2= NFPGVFdFVVOR NHf1d2xqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhTUeIUjDhcoQhSWu2 NFW1WGcyPzZ6OUK4OS=>
HSC-2 M3joSWFxd3C2b4Ppd{Bie3OjeR?= MmTxPOKh|ryP MWnEUXNQ NXjTelRXcW6qaXLpeJMhTmG|LX3l[IlifGWmIHHwc5B1d3Orcx?= M1:3OVE4Pjh7Mki1
HEp-2 NWPr[pprT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWH+NVAh|ryP MYLEUXNQ M1vOV4VvcGGwY3XzJI9zcWSxbnnuMYlv\HWlZXSg[5Jwf3SqLXnubIljcXSxcom= M1vQVVIxOjB{N{Sx
SubG1 NYLH[5I1SXCxcITvd4l{KGG|c3H5 MlPUglExKM7:TR?= MYjEUXNQ MVXlcohidmOnczDvdolld26rbj3pcoR2[2WmIHHwc5B1d3Orcx?= MYSyNFIxOjd2MR?=
HEp-2 M4TiXmZ2dmO2aX;uJIF{e2G7 NXP1bXQ5hjFyIN88US=> NVXrR5JRTE2VTx?= NVjlbpFm\W6qYX7j[ZMhV3KrZH;ubY4ucW6mdXPl[EBD[XhiYXP0bZZifGmxbjygRoNtNTJiZHXndoFl[XSrb36gZY5lKFOLUmSxJIlv[WO2aY\heIlwdg>? MX6yNFIxOjd2MR?=
H508 NYjIbmNXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NELMflF,OSEQvF2= M2TId2ROW09? M2\tfY1qfGmpYYTld{BEWEZvbXXkbYF1\WRiSEWwPEBk\WyuIHfyc5d1cA>? NVK4SXY6OjZ3MUS5NlQ>

... Click to View More Cell Line Experimental Data

In vivo試験 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]

プロトコル (参考用のみ)



細胞株 U87MG
濃度 Dissolved in DMSO, final concentrations ~100 μM
反応時間 72 hours

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.



動物モデル Female BALB/c nu/nu mice inoculated s.c. with A431 or U87MG.Δ2-7 tumor cells
製剤 Dissolved in 100 mM Captisol
投薬量 ~1 mg/kg
投与方法 Injection i.p. three times per week

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)



Download AG-1478 (Tyrphostin AG-1478) SDF
分子量 315.75


CAS No. 153436-53-4
保管 3年-20℃
2年-80℃in solvent
別名 NSC 693255
溶解度 (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.
化学名 N-(3-chlorophenyl)-6,7-dimethoxyquinazolin-4-amine

文献中の引用 (7)



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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID