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Synonyms | Tyrphostin AG-1478, NSC 693255 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C16H14ClN3O2 |
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分子量 | 315.75 | CAS No. | 153436-53-4,175178-82-2 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 25 mg/mL (79.17 mM) | ||||||||
Ethanol | 13 mg/mL (41.17 mM) | ||||||||||
Water | Insoluble | ||||||||||
体内 (毎回新しく調製した物を用意してください) |
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* <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. |
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). |
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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] |
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] |
細胞アッセイ | 細胞株 | U87MG |
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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. |
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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 |
投薬量 | ~1 mg/kg | |
投与方法 | Injection i.p. three times per week |
Data from [Data independently produced by Biomed Pharmacother, 2014, 10.1016/j.biopha.2014.09.003]
Data from [Data independently produced by Toxicol Lett, 2014, 226(1), 81-9]
Data from [Data independently produced by , , PLoS One, 2013, 8(8): e70353]
Calpain-2 mediates SARS-CoV-2 entry via regulating ACE2 levels [ mBio, 2024, e0228723.] | PubMed: 38349185 |
Biliary epithelial cells are facultative liver stem cells during liver regeneration in adult zebrafish [ JCI Insight, 2023, 8(1)e163929] | PubMed: 36625346 |
Revitalizing Skin Repair: Unveiling the Healing Power of Livisin, a Natural Peptide Calcium Mimetic [ Toxins (Basel), 2023, 16(1)21] | PubMed: 38251238 |
Argininosuccinate lyase drives activation of mutant TERT promoter in glioblastomas [ Mol Cell, 2022, 82(20):3919-3931.e7] | PubMed: 36270249 |
Fluorescent Biosensor for Measuring Ras Activity in Living Cells [ J Am Chem Soc, 2022, 144(38):17432-17440] | PubMed: 36122391 |
ITGB4 deficiency induces mucus hypersecretion by upregulating MUC5AC in RSV-infected airway epithelial cells [ Int J Biol Sci, 2022, 18(1):349-359] | PubMed: 34975337 |
SMGL-1/NBAS acts as a RAB-8 GEF to regulate unconventional protein secretion [ J Cell Biol, 2022, 221(7)e202111125] | PubMed: 35604368 |
RNA N6-methyladenosine modulates endothelial atherogenic responses to disturbed flow in mice [ Elife, 2022, 11e69906] | PubMed: 35001873 |
ITGB4 Deficiency in Airway Epithelium Aggravates RSV Infection and Increases HDM Sensitivity [ Front Immunol, 2022, 13:912095] | PubMed: 35958591 |
Lysophosphatidic acid suppresses apoptosis of high-grade serous ovarian cancer cells by inducing autophagy activity and promotes cell-cycle progression via EGFR-PI3K/Aurora-AThr288-geminin dual signaling pathways [ Front Pharmacol, 2022, 13:1046269] | PubMed: 36601056 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。