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



Quality Control & MSDS


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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]
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 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

カスタマーフィードバック (3)

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Source Toxicol Lett, 2014, 226(1), 81-9. AG-1478 (Tyrphostin AG-1478) purchased from Selleck
Method Western blot
Cell Lines TM4 cells
Concentrations 10 uM
Incubation Time 15 min
Results Phosphorylation of ERK1/2 caused by exposure to BPA was abolished in the presence of G15, PD 98059, or AG 1478 alone or in combination of all three antagonists together, suggesting that GPR30 and EGFR signaling is required for ERK1/2 activation after exposure to BPA and consequently for BPA-induced TM4 cell proliferation.

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Source , , PLoS One, 2013, 8(8): e70353. AG-1478 (Tyrphostin AG-1478) purchased from Selleck
Method Microscope Imaging & Western Blot
Cell Lines HeLa, CaSki, SiHa cells
Concentrations 5 μM
Incubation Time 24 h
Results Treatment with 5 μM of AG1478 abolished EGF-induced morphological changes (Figure A) and TACC3 induction (Figure B), and as a consequence, EGF-mediated EMT was inhibited (Figure B). This data suggests that activation of EGFR is required for EGF-mediated TACC3 induction.

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Source Biomed Pharmacother, 2014, 10.1016/j.biopha.2014.09.003. AG-1478 (Tyrphostin AG-1478) purchased from Selleck
Method Western blot
Cell Lines A549 cells
Concentrations 10 uM
Incubation Time 15 min
Results Maximum phosphorylation of ERK1/2 was reached at 10–15 min. Further, both G15 (the specific inhibitor of GPER) and AG 1478 (the specific inhibitor of EGFR) significantly abolished the BPA induced activation of ERK1/2 in A549 cells.

文献中の引用 (7)



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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID