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受注：045-509-1970 |
技術サポート：[email protected] 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 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C22H23N3O4 |
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| 分子量 | 393.44 | CAS No. | 183321-74-6 | |
| Solubility (25°C)* | 体外 | DMSO | 78 mg/mL (198.25 mM) | |
| Ethanol | 21 mg/mL warmed with 50ºC water bath (53.37 mM) | |||
| Water | 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 is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib induces autophagy. |
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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 human colon cancer cells and MDA MB-468 human breast cancer cells. Erlotinib HCl (1 μM) induces apoptosis in DiFi human colon cancer cells. [1] Erlotinib 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. [2] Erlotinib HCl(2 μM) significantly inhibits growth of AsPC-1 and BxPC-3 pancreatic cells. [3] The effects of Erlotinib HCl in combination with gemcitabine are considered additive in KRAS-mutated pancreatic cancer cells. Ten micromolar of Erlotinib HCl inhibits EGFR phospho-rylation at the Y845 (Src-dependent phosphorylation) and Y1068 (auto-phosphorylation) sites. [4] Combination with Erlotinib HCl could down-modulate rapamycin-stimulated Akt activity and produces a synergistic effect on cell growth inhibition. [5] |
| 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. [1] Erlotinib HCl (100 mg/Kg) inhibits H460a and A549 tumor models with 71 and 93% inhibition rate. [5] |
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 colorimetric 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 drug(s) compared with untreated control cells and is calculated by the CalcuSyn software. |
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| 動物実験 | 動物モデル | Male 5-week-old BALB-nu/nu mice with HPAC cells |
| 投薬量 | 50 mg/kg | |
| 投与方法 | Oral administration | |
参考
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 [Head Neck, 2013, 35, 86-93]
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Data from [Tuberc Respir Dis, 2013, 75(1), 9-17]
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：
| Tet methylcytosine dioxygenase 2 (TET2) deficiency elicits EGFR-TKI (tyrosine kinase inhibitors) resistance in non-small cell lung cancer [ Signal Transduct Target Ther, 2024, 9(1):65] | PubMed: 38461173 |
| Activation of the PI3K/AKT signaling pathway by ARNTL2 enhances cellular glycolysis and sensitizes pancreatic adenocarcinoma to erlotinib [ Mol Cancer, 2024, 23(1):48] | PubMed: 38459558 |
| Comprehensive mutational scanning of EGFR reveals TKI sensitivities of extracellular domain mutants [ Nat Commun, 2024, 15(1):2742] | PubMed: 38548752 |
| TWIST1 is a critical downstream target of the HGF/MET pathway and is required for MET driven acquired resistance in oncogene driven lung cancer [ Oncogene, 2024, 10.1038/s41388-024-02987-5] | PubMed: 38485737 |
| A destabilizing Y891D mutation in activated EGFR impairs sensitivity to kinase inhibition [ NPJ Precis Oncol, 2024, 8(1):3] | PubMed: 38182677 |
| Mobocertinib in Patients with EGFR Exon 20 Insertion-Positive Non-Small Cell Lung Cancer (MOON): An International Real-World Safety and Efficacy Analysis [ Int J Mol Sci, 2024, 25(7)3992] | PubMed: 38612799 |
| Non-small cell lung cancer cells with uncommon EGFR exon 19delins variants respond poorly to third-generation EGFR inhibitors [ Transl Oncol, 2024, 39:101834] | PubMed: 38006760 |
| Extracellular domain mutations of the EGF receptor differentially modulate high affinity and low affinity responses to EGF receptor ligands [ J Biol Chem, 2024, S0021-9258(24)00139-X] | PubMed: 38367671 |
| HER3 overexpression: a predictive marker for poor prognosis in advanced ALK-positive non-small cell lung cancer treated with ALK inhibitors [ Transl Lung Cancer Res, 2024, 13(2):321-333] | PubMed: 38496685 |
| Transgelin-2, a novel cancer stem cell-related biomarker, is a diagnostic and therapeutic target for biliary tract cancer [ BMC Cancer, 2024, 24(1):357] | PubMed: 38509504 |
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。