受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C27H31N7O2 |
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分子量 | 485.58 | CAS No. | 1421373-98-9 | |
Solubility (25°C)* | 体外 | DMSO | 97 mg/mL (199.76 mM) | |
Ethanol | 2 mg/mL warmed with 50ºC water bath (4.11 mM) | |||
Water | Insoluble | |||
* <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 | AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor with IC50 of <1 nM, 6 nM, 1 nM, and 25 nM for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively. Phase 1. |
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in vitro | AZ5104 shows great potency against ex19del (2 nM in PC-9), T790M (2 nM in H1975), and wild-type EGFR (33 nM in LOVO) cell lines. AZ5104 causes inhibition of cell viability with IC50 of 3.3 nM, 2.6 nM, 80 nM, and 53 nM for H1975 (T790M/L858R), PC-9 (ex19del), Calu 3 (WT), and NCI-H2073 (WT), respectively. [1] |
in vivo | In both C/L858R and C/L+T mice, AZ5104 (5 mg/kg/d, p.o.) induces significant and sustained tumor regression. [1] |
キナーゼアッセイ | Recombinant Kinase assays | |
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Kinase assays are performed using peptide or protein substrates in a filter-binding radioactive ATP transferase assay for protein kinases, or lipid substrates and HTRF assay for lipid kinase. | ||
細胞アッセイ | 細胞株 | H1975 (T790M/L858R), PC-9 (ex19del), Calu 3 (WT), and NCI-H2073 (WT) cells |
濃度 | ||
反応時間 | 96 h | |
実験の流れ | Growth-inhibition assays are performed using CellTiter Blue Reagent, and IC50 values are calculated using Excel. | |
動物実験 | 動物モデル | Mice bearing C/L858R and C/L+T tumors |
投薬量 | 5 mg/kg/d | |
投与方法 | p.o. |
Bioanalysis of EGFRm inhibitor osimertinib, and its glutathione cycle- and desmethyl metabolites by liquid chromatography-tandem mass spectrometry. [ J Pharm Biomed Anal, 2020, 177:112871] | PubMed: 31539712 |
YH25448, an Irreversible EGFR-TKI with Potent Intracranial Activity in EGFR Mutant Non-Small Cell Lung Cancer [ Clin Cancer Res, 2019, 25(8):2575-2587] | PubMed: 30670498 |
Electrotaxis of Glioblastoma and Medulloblastoma Spheroidal Aggregates. [ Sci Rep, 2019, 9(1):5309] | PubMed: 30926929 |
Activity of a novel HER2 inhibitor, poziotinib, for HER2 exon 20 mutations in lung cancer and mechanism of acquired resistance: An in vitro study. [ Lung Cancer, 2018, 126:72-79] | PubMed: 30527195 |
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。