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

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製品説明

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    EGFR製品生物活性の比較
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製品の説明

生物活性

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。
ターゲット

EGFR

IC50

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 NGDFSWVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWH+NVAxKM7:TR?= NFXuS49FVVOR NXvIZ|NwUUN3ME2zOE43KM7:TR?= MYO4O|UzOTR3
U87MG.ΔEGFR NFrzXXZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHvPSY9,OTByIN88US=> NU\yPJpzTE2VTx?= MYfJR|UxRThwNzFOwG0> NXnp[4luQDd3MkG0OS=>
U87MG.wtEGFR. M4LMRWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{n6ZZ4yODBizszN NHzYU|BFVVOR MXrJR|UxRTR6LkSg{txO M{TLZVg4PTJzNEW=
U87MG M2i1bWtqdmG|ZTDhd5NigQ>? M4PTR54yODBizszN NVzVV3ViTE2VTx?= M1ezUIlvcGmkaYTzJGVITlJidInyc5NqdmVia3nuZZNmKGGldHn2bZR6 M1nBb|g4PTJzNEW=
U87MG.ΔEGFR NEHTWXlMcW6jc3WgZZN{[Xl? MWH+NVAxKM7:TR?= Mme4SG1UVw>? MVTpcohq[mm2czDFS2ZTKHS7cn;zbY5mKGurbnHz[UBi[3Srdnn0fS=> NHH3NXA5PzV{MUS1
U87MG.wtEGFR. MnjuT4lv[XOnIHHzd4F6 NHfVXYt,OTByIN88US=> MULEUXNQ NYO5RotCcW6qaXLpeJMhTUeIUjD0fZJwe2mwZTDrbY5ie2ViYXP0bZZqfHl? M{PHPVg4PTJzNEW=
HPV 16-immortalized human keratinocytes MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoHSglUxKM7:TR?= MV7EUXNQ NEmxW3hqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M1XVflkzQDh5OEK=
HPV 16-immortalized human keratinocytes NFjadJhHfW6ldHnvckBie3OjeR?= MknBglUxKM7:TR?= MYrEUXNQ MmLubY5lfWOnczDhdpJme3RiaX6geIhmKEOnbHygR5lkdGV? M3Xic|kzQDh5OEK=
HPV 16-immortalized human keratinocytes NFnNNFdCeG:ydH;zbZMh[XO|YYm= MYX+OVAh|ryP MUnEUXNQ NWnvO5pZcW6mdXPld{BieG:ydH;zbZMv MUC5Nlg5Pzh{
A431 NIm5UZlMcW6jc3WgZZN{[Xl? MUP+NVAh|ryP NXfMdVNWTE2VTx?= NXTPd3dYcW6qaXLpeJMhfGinIHLhd4FtKGGwZDDUS2Yu|rFvc4TpcZVt[XSnZDD0fZJwe2mwZTDwbI9{eGixconsZZRqd25ib3[geIhmKEWJRmK= NVjpWJRTOTB5MEKyOlI>
MDA-468  NIT4NGJMcW6jc3WgZZN{[Xl? MYr+NVAh|ryP NXTBdnRVTE2VTx?= M{fBNYlvcGmkaYTzJJRp\SCkYYPhcEBidmRiVFfGMe6yNXO2aX31cIF1\WRidInyc5NqdmVicHjvd5Bpd3K7bHH0bY9vKG:oIITo[UBGT0[U MVOxNFcxOjJ4Mh?=
A431 Mm\mSpVv[3Srb36gZZN{[Xl? M2m4U54yOCEQvF2= M2WzO2ROW09? MYLpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 Mkj2NVA4ODJ{NkK=
MDA-MB-231 M4PXTGtqdmG|ZTDhd5NigQ>? M1vKT542KM7:TR?= NEPTb|NFVVOR MoG2bY5pcWKrdIOgSWdHKHO2aX31cIF1\WRicHjvd5Bpd3K7bHH0bY9vKG:oIF\LTHI> MoT4NVExOzBzNE[=
CNE2 MoKxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXLwT|dmOTByIN88US=> MoHoSG1UVw>? NF3lVplqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[nliOUiuOEU> MV[xNVQyODN{Mh?=
CNE2 M1KzT2tqdmG|ZTDhd5NigQ>? M{HLfJ4yODBizszN NH7lS2FFVVOR NUDMO|kxcW6qaXLpeJMhTUeIUjD0fZJwe2mwZTDwbI9{eGixconsZZRqd25? M4LjNlEyPDFyM{Ky
CNE2 NGXX[IdHfW6ldHnvckBie3OjeR?= MknQglExOCEQvF2= MYLEUXNQ NWT2[GVjUW6qaXLpeJMhVUGSSzDhcoQhSUuWIHHjeIl3[XSrb36= MWGxNVQyODN{Mh?=
CNE2 MVPGeY5kfGmxbjDhd5NigQ>? NYrndJN{hjVyIN88US=> NGXqSGFFVVOR M{L5WoFn\mWldIOgZ4VtdCCleXPs[UBlcXO2cnnieZRqd25? MYKxNVQyODN{Mh?=
HSC-2 MVPLbY5ie2ViYYPzZZk> NYnKNHRFQMLizszN NYnkcVBpTE2VTx?= NUnnRpl1cW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEWJRmKgZY5lKEGtdB?= NFzzNWcyPzZ6OUK4OS=>
HSC-2 MVTBdI9xfG:|aYOgZZN{[Xl? NUPYVYM3QMLizszN Mn3QSG1UVw>? NGq5ZWVqdmirYnn0d{BH[XNvbXXkbYF1\WRiYYDvdJRwe2m| M1rqcFE4Pjh7Mki1
HEp-2 NXvLfYZOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGPEcmZ,OTBizszN MnzCSG1UVw>? NFfLcoFmdmijbnPld{Bwemmmb37pck1qdmS3Y3XkJIdzd3e2aD3pcohq[mm2b4L5 NHqwZ2ozODJyMke0NS=>
SubG1 Mof2RZBweHSxc3nzJIF{e2G7 MUn+NVAh|ryP M1Pj[WROW09? Mnrk[Y5p[W6lZYOgc5Jq\G:waX6tbY5lfWOnZDDhdI9xfG:|aYO= M1HxV|IxOjB{N{Sx
HEp-2 NH31UGZHfW6ldHnvckBie3OjeR?= MYX+NVAh|ryP MVzEUXNQ NEWw[mhmdmijbnPld{BQemmmb37pck1qdmS3Y3XkJGJigCCjY4TpeoF1cW:wLDDCZ4wuOiCmZXfyZYRifGmxbjDhcoQhW0mUVEGgbY5i[3SrdnH0bY9v MUKyNFIxOjd2MR?=
H508 NWXvOJQ3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFe2dFR,OSEQvF2= NGPa[JdFVVOR MVftbZRq\2G2ZYOgR3BHNW2nZHnheIVlKEh3MEigZ4VtdCCpcn;3eIg> NVnDbFhLOjZ3MUS5NlQ>

... 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]
臨床試験
特集

プロトコル (参考用のみ)

細胞アッセイ:

[2]

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

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.

動物実験:

[4]

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)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
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)
1

参考

化学情報

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

C16H14ClN3O2

CAS No. 153436-53-4
保管 2年-20℃
6月-80℃in solvent
別名 NSC 693255
溶解度 (25°C) * In vitro DMSO 25 mg/mL (79.17 mM)
エタノール 13 mg/mL (41.17 mM)
<1 mg/mL (<1 mM)
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
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