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受注：045-509-1970 |
技術サポート：tech@selleck.co.jp 平日9:00〜18:00 1営業日以内にご連絡を差し上げます |
化学情報
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Synonyms | CP358774, NSC 718781,OSI-774 HCl | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C22H23N3O4.HCl |
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| 分子量 | 429.90 | CAS No. | 183319-69-9 | |
| Solubility (25°C)* | 体外 | DMSO | 6 mg/mL (13.95 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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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. |
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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | Erlotinib HCl は、細胞を含まないアッセイで IC50 が 2 nM の EGFR 阻害剤であり、ヒト c-Src または v-Abl よりも EGFR に対して 1000 倍以上感度が高いです。 |
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| in vitro | Erlotinib HCl potently inhibits EGFR activation in intact cells including HNS human head and neck tumor cells (IC50 20nM), DiFi humancolon cancer cells andMDA MB-468 human breast cancer cells. This compound (1 μM) induces apoptosis in DiFi humancolon cancer cells. It inhibits growth of a panel of NSCLC cell lines including A549, H322, H3255, H358 H661, H1650, H1975, H1299, H596 with IC50 ranging from 29 nM to >20 μM. This chemical (2 μM) significantly inhibits growth of AsPC-1 and BxPC-3 pancreatic cells. The effects of this compound in combination with gemcitabine are considered additive in KRAS-mutated pancreatic cancer cells. Ten micromolar of this chemical inhibits EGFR phospho-rylation at the Y845 (Src-dependent phosphorylation) and Y1068 (auto-phosphorylation) sites. Combination with it could down-modulate rapamycin-stimulated Akt activity and produces a synergistic effect on cell growth inhibition. |
| in vivo | At doses of 100 mg/kg, Erlotinib HCl completely prevents EGF-induced autophosphorylation of EGFR in human HN5 tumors growing as xenografts in athymic mice and of the hepatic EGFR of the treated mice. This compound (100 mg/Kg) inhibits H460a and A549 tumor models with 71 and 93% inhibition rate. |
プロトコル(参考用のみ)
| キナーゼアッセイ | Kinase assays | |
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| 96-well plates are coated by incubation overnight at 37 °C with 100 μL per well of 0.25 mg/mL PGT in PBS. Excess PGT is removed by aspiration, and the plate is washed 3 times with washing buffer (0.1% Tween 20 in PBS). The kinase reaction is performed in 50 μL of 50 mM HEPES (pH 7.3), containing 125 mM sodium chloride, 24 mM magnesium chloride, 0.1 mM sodium orthovanadate, 20 μM ATP, 1.6 μg/mL EGF, and 15 ng of EGFR, affinity purified from A431 cell membranes. Erlotinib HCl in DMSO is added to give a final DMSO concentration of 2.5%. Phosphorylation is initiated by addition of ATP and proceeded for 8 minutes at room temperature, with constant shaking. The kinase reaction is terminated by aspiration of the reaction mixture and is washed 4 times with washing buffer. Phosphorylated PGT is measured by 25 minutes of incubation with 50 μL per well HRP-conjugated PY54 antiphosphotyrosine antibody, diluted to 0.2 μg/mL in blocking buffer (3% BSA and 0.05% Tween 20 in PBS). Antibody is removed by aspiration, and the plate is washed 4 times with washing buffer. The colonmetric signal is developed by addition of TMB Microwell Peroxidase Substrate, 50μL per well, and stopped by the addition of 0.09 M sulfuric acid, 50 μL per well. Phosphotyrosine is estimated by measurement of absorbance at 450 nm. The signal for controls is typically 0.6-1.2 absorbance units, with essentially no back ground in wells without AlP, EGFR, or PGT and is proportional to the time of incubation for 10 minutes. | ||
| 細胞アッセイ | 細胞株 | A549, H322, H3255, H358 H661, H1650, H1975, H1299, H596 cells |
| 濃度 | 30 nM-20 μM | |
| 反応時間 | 72 hours | |
| 実験の流れ | Exponentially growing cells are seeded in 96-well plastic plates and exposed to serial dilutions of erlotinib, pemetrexed, or the combination at a constant concentration ratio of 4:1 in triplicates for 72 h. Cell viability is assayed by cell count and the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Growth inhibition is expressed as the percentage of surviving cells in drug-treated versus PBS-treated control cells (which is considered as 100% viability). The IC50 value is the concentration resulting in 50% cell growth inhibition by a 72-h exposure to this compound compared with untreated control cells and is calculated by the CalcuSyn software. | |
| 動物実験 | 動物モデル | Male 5-week-old BALB-nu/nu with HPAC cells |
| 投薬量 | 50 mg/kg | |
| 投与方法 | Oral administration | |
参考
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カスタマーフィードバック
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Data from [Cancer Res, 2014, 4(1):253-62]
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Data from [Tuberc Respir Dis, 2013, 75(1), 9-17]
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Data from [Head Neck, 2013, 35, 86-93]
Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：
| Lysosomal EGFR acts as a Rheb-GEF independent of its kinase activity to activate mTORC1 [ Cell Res, 2025, 10.1038/s41422-025-01110-x] | PubMed: 40259053 |
| Identifying potential risk genes for clear cell renal cell carcinoma with deep reinforcement learning [ Nat Commun, 2025, 16(1):3591] | PubMed: 40234405 |
| Reciprocal regulation of MMP-28 and EGFR is required for sustaining proliferative signaling in PDAC [ J Exp Clin Cancer Res, 2025, 44(1):68] | PubMed: 39994761 |
| Integration of 3D bioprinting and multi-algorithm machine learning identified glioma susceptibilities and microenvironment characteristics [ Cell Discov, 2024, 10(1):39] | PubMed: 38594259 |
| RAB22A sorts epithelial growth factor receptor (EGFR) from early endosomes to recycling endosomes for microvesicles release [ J Extracell Vesicles, 2024, 13(7):e12494] | PubMed: 39051763 |
| Metabolic imaging distinguishes ovarian cancer subtypes and detects their early and variable responses to treatment [ Oncogene, 2024, 10.1038/s41388-024-03231-w] | PubMed: 39639170 |
| Hepatocellular RECK as a Critical Regulator of Metabolic Dysfunction-Associated Steatohepatitis Development [ Cell Mol Gastroenterol Hepatol, 2024, S2352-345X(24)00119-X] | PubMed: 38797477 |
| Establishment, characterization, and biobanking of 36 pancreatic cancer organoids: prediction of metastasis in resectable pancreatic cancer [ Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5] | PubMed: 38619751 |
| The deubiquitinase USP9X regulates RIT1 protein abundance and oncogenic phenotypes [ iScience, 2024, 27(8):110499] | PubMed: 39161959 |
| Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862] | PubMed: 39319271 |
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。