AG-1478

別名:Tyrphostin AG-1478, NSC 693255

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. AG-1478 (Tyrphostin AG-1478) inhibits encephalomyocarditis virus (EMCV) and hepatitis c virus (HCV) by targeting phosphatidylinositol 4-kinase IIIα (PI4KA).

AG-1478化学構造

CAS No. 153436-53-4,175178-82-2

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 13300 国内在庫あり
JPY 13600 国内在庫あり
JPY 38500 国内在庫あり

代表番号: 045-509-1970|電子メール:[email protected]
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文献中Selleckの製品使用例(89)

製品安全説明書

現在のバッチを見る: S272801 DMSO] 25 mg/mL] false] Ethanol] 13 mg/mL] false] Water] Insoluble] false 純度: 99.92%
99.92

AG-1478関連製品

シグナル伝達経路

EGFR阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
A431 Function assay ~10 μM induces cell cycle arrest 10702262
MDA-468  Kinase assay ~10 μM inhibits the basal and TGF-α-stimulated tyrosine phosphorylation of the EGFR 10702262
A431 Kinase assay ~10 μM inhibits the basal and TGF-α-stimulated tyrosine phosphorylation of the EGFR 10702262
HPV 16-immortalized human keratinocytes Apoptosis assay ~50 μM induces apoptosis. 9288782
HPV 16-immortalized human keratinocytes Function assay ~50 μM induces arrest in the Cell Cycle 9288782
HPV 16-immortalized human keratinocytes Growth inhibitory assay ~50 μM inhibits cell growth 9288782
U87MG.wtEGFR. Kinase assay ~100 μM inhibits EGFR tyrosine kinase activity 8752145
U87MG.ΔEGFR Kinase assay ~100 μM inhibits EGFR tyrosine kinase activity 8752145
U87MG Kinase assay ~100 μM inhibits EGFR tyrosine kinase activity 8752145
U87MG.wtEGFR. Growth inhibitory assay ~100 μM IC50=48.4 μM 8752145
U87MG.ΔEGFR Growth inhibitory assay ~100 μM IC50=8.7 μM 8752145
U87MG Growth inhibitory assay ~100 μM IC50=34.6 μM 8752145
MDA-MB-231 Kinase assay ~5 μM inhibits EGF stimulated phosphorylation of FKHR 11030146
CNE2 Growth inhibitory assay 100 μM inhibits cell proliferation by 98.4% 11410322
CNE2 Kinase assay ~100 μM inhibits EGFR tyrosine phosphorylation 11410322
CNE2 Function assay ~100 μM Inhibits MAPK and AKT activation 11410322
CNE2 Function assay ~50 μM affects cell cycle distribution 11410322
HSC-2 Kinase assay 8 μM inhibits phosphorylation of EGFR and Akt 17689285
HSC-2 Apoptosis assay 8 μM inhibits Fas-mediated apoptosis 17689285
HEp-2 Growth inhibitory assay ~10 μM enhances oridonin-induced growth-inhibitory 20202741
SubG1 Apoptosis assay ~10 μM enhances oridonin-induced apoptosis 20202741
HEp-2 Function assay ~10 μM enhances Oridonin-induced Bax activation, Bcl-2 degradation and SIRT1 inactivation 20202741
H508 Growth inhibitory assay ~1 μM mitigates CPF-mediated H508 cell growth 26514924
HeLa Function assay 30 mins Inhibition of EGFR autophosphorylation in human HeLa cells preincubated for 30 mins prior to EGF stimulation by Western blotting 21718029
HEK293 Function assay 1 hr Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, Ki=1.87μM 29941193
HEK293 Function assay 1 hr Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, IC50=19.6μM 29941193
A431 Antiproliferative assay Tested for antiproliferative activity against human A431 cells, IC50=20μM 15109642
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
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生物活性

製品説明 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. AG-1478 (Tyrphostin AG-1478) inhibits encephalomyocarditis virus (EMCV) and hepatitis c virus (HCV) by targeting phosphatidylinositol 4-kinase IIIα (PI4KA).
Targets
EGFR [1]
(Cell-free assay)
3 nM
In Vitro
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]
細胞実験 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.

実験結果図 Methods Biomarkers 結果図 PMID
Growth inhibition assay Cell viability 25258648
Western blot Shc / PLC-γ1 EGFR / Neu / p-Tyr 10931950
In Vivo
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]
動物実験 動物モデル Female BALB/c nu/nu mice inoculated s.c. with A431 or U87MG.Δ2-7 tumor cells
投与量 ~1 mg/kg
投与経路 Injection i.p. three times per week

化学情報

分子量 315.75 化学式

C16H14ClN3O2

CAS No. 153436-53-4,175178-82-2 SDF Download AG-1478 SDFをダウンロードする
Smiles COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=CC=C3)Cl)OC
保管

In vitro
Batch:

DMSO : 25 mg/mL ( (79.17 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 13 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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Handling Instructions

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