AG-1478 (Tyrphostin AG-1478)

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。

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



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情報 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]
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]

推薦された実験操作 (公開の文献だけ)



細胞系 U87MG
濃度 Dissolved in DMSO, final concentrations ~100 μM
処理時間 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
管理 Injection i.p. three times per week



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


CAS No. 153436-53-4
別名 N/A
溶解度 (25°C)
  • DMSO 25 mg/mL
  • 水 <1 mg/mL
  • エタノール 13 mg/mL
保管 2年 -20°C
6月-80°Cin DMSO
化学名 N-(3-chlorophenyl)-6,7-dimethoxyquinazolin-4-amine


カスタマーレビュー (2)

Click to enlarge
Source , , PLoS One. 2013 Aug 1;8(8):e70353 . AG-1478 (Tyrphostin AG-1478) purchased from Selleck
Method Western blot
Cell Lines EGFR-expressing cells
Concentrations 5 uM
Incubation Time 24 h
Results Treatment with 5 μM of AG1478 abolished EGF-induced morphological changes and TACC3 induction , and as a consequence, EGF-mediated EMT was inhibited.

Click to enlarge
Source , , PLoS One. 2013 Aug 1;8(8):e70353 . AG-1478 (Tyrphostin AG-1478) purchased from Selleck
Method microscope imaging
Cell Lines EGFR-expressing cells
Concentrations 5 uM
Incubation Time 24 h
Results Treatment with 5 μM of AG1478 abolished EGF-induced morphological changes and TACC3 induction.

製品表彰状 (4)

  • TACC3 Is Essential for EGF-Mediated EMT in Cervical Cancer. [Geun-Hyoung Ha, et al. PLoS ONE 2013;8(8): e70353]

    PubMed: 23936413
  • Involvement of activating ERK1/2 through G protein coupled receptor 30 and estrogen receptor α/β in low doses of bisphenol A promoting growth of Sertoli TM4 cells [Ge LC Toxicol Lett 2014;10.1016/j.toxlet.2014.01.035]

    PubMed: 24495410
  • Opposing Effect of EGFRWT on EGFRvIII-Mediated NF-κB Activation with RIP1 as a Cell Death Switch. [Puliyappadamba VT, et al. Cell Rep 2013;4(4):764-75]

    PubMed: 23972990
  • Rab25 Small GTPase Mediates Secretion of Tumor Necrosis Factor Receptor Superfamily Member 11b (osteoprotegerin) Protecting Cancer Cells from Effects of TRAIL. [Cheng KW, et al. Genetic Syndromes & Gene Therapy 2013;4:6]



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