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化学名: | ネラチニブ | 英語化学名: | Neratinib | 别名: | Neratinib(HKI-272);(2E)-N-[4-[[3-chloro-4-(2-pyridinylMethoxy)phenyl]aMino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(diMethylaMino)-2-butenaMide;neratinib;(E)-N-[4-[3-Chloro-4-[(2-pyridinyl)methoxy]anilino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide;N-(4-(3-Chloro-4-(2-pyridinylmethoxy)anilino)-3-cyano-7-ethoxy-6-quinolyl)-4-(dimethylamino)-2-butenamide;Unii-jjh94R3pwb;(2e)-n-(4-((3-chloro-4-((pyridin-2-yl)Methoxy)phenyl)aMino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(diMethylaMino)but-2-enaMide neratinib;HKI-272 Neratinib | CAS番号: | 698387-09-6 | 分子式: | C30H29ClN6O3 | 分子量: | 557.04 | EINECS: | 811-237-1 | カテゴリ情報: | Inhibitors;Anti-cancer & immunity;Antineoplastic;API | Mol File: | 698387-09-6.mol | |
融点 | 185-187°C | 沸点 | 757.0±60.0 °C(Predicted) | 比重(密度) | 1.33 | 貯蔵温度 | Refrigerator | 溶解性 | Chloroform (Slightly), DMSO (Slightly, Heated, Sonicated), Methanol (Slightly, Heated) | 外見 | Off-white solid. | 酸解離定数(Pka) | 12.37±0.43(Predicted) | 色 | Pale Yellow to Yellow |
| ネラチニブ Usage And Synthesis |
効能 | 抗悪性腫瘍薬, 受容体チロシンキナーゼ阻害薬 | 説明 | The receptor tyrosine kinase HER2 (ErbB2) is a key component of epidermal growth factor receptor complexes that are known to have central roles in cell proliferation and cancer. Neratinib is an orally active, irreversible inhibitor of the HER2 kinase (IC50 = 59 nM). It also potently inhibits several mutants of HER2 and shows 10-fold or greater selectivity over a wide variety of other kinases. As an irreversible inhibitor, neratinib may circumvent acquired resistance developed against reversible inhibitors, including gefitinib . Neratinib has been evaluated in clinical trials against cancers characterized by HER2 overexpression or HER2 activating mutations. | 使用 | An oral, irreversible dual EGFR/HER2 inhibitor for breast and non-small cell lung cancer. Antitumor agent. | 使用 | Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM, respectively. | 定義 | ChEBI: A quinoline compound having a cyano group at the 3-position, a 3-chloro-4-(2-pyridylmethoxy)anilino group at the 4-position, a 4-dimethylamino-trans-but-2-enamido group at the 6-position, and an ethoxy group at the 7-position. | target | HER2 | 貯蔵 | Store at -20°C |
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