USD $25.00-50.00 / Metric Ton
USD $8.20-8.80 / Kilogram
USD $8.20-8.80 / Kilogram
USD $8.20-8.80 / Kilogram
USD $25.00-50.00 / Metric Ton
neratinib basic information |
product name: | neratinib |
synonyms: | (2e)-n-[4-[[3-chloro-4-[(pyridin-2-yl)methoxy]phenyl]amino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide;neratinib;(e)-n-[4-[3-chloro-4-[(2-pyridinyl)methoxy]anilino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide;(2e)-n-[4-[[3-chloro-4-[(pyridin-2-yl)methoxy]phenyl]amino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide;n-(4-(3-chloro-4-(2-pyridinylmethoxy)anilino)-3-cyano-7-ethoxy-6-quinolyl)-4-(dimethylamino)-2-butenamide;unii-jjh94r3pwb;neratinib(hki-272);(2e)-n-[4-[[3-chloro-4-(2-pyridinylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide |
cas: | 698387-09-6 |
mf: | c30h29cln6o3 |
mw: | 557.04266 |
einecs: | |
product categories: | antineoplastic;anti-cancer & immunity;inhibitors |
mol file: | 698387-09-6.mol |
neratinib chemical properties |
density | 1.33 |
safety information |
neratinib usage and synthesis |
new anticancer drug |
neratinib developed by us wyeth company is an irreversible epidermal growth factor receptor(egfr) inhibitor. it is a multiple target point of small molecule tyrosine kinase inhibitors to her 2 and her1 after lapatinib, and is an irreversible erbb receptor tyrosine kinase inhibitor. neratinib could selectively inhibit her-1 and her-2 of egfr family(ic50 was 92 nmol/l and 59 nmol/l, respectively). clinical research showed that neratinib exerted significant therapeutic effect on non-small cell lung cancer, colon cancer, and breast cancer. the phaseⅱclinical trial indicated that neratinib showed good efficacy and tolerance to her-2 positive patients with advanced breast cancer who had been received or not trastuzumab treatment. the phase ⅲ breast cancer clinical trial was complete in september 2014. the data indicated that the efficacy of neratinib was better than roche's herceptin in treatment of her-2 positive early breast cancer. the above information is edited by the chemicalbook of liu yujie. |
synthesis pathways |
3-chloro-4- (pyridin-2-yl-methoxy) - aniline (2) and n- (4- chloro-3-cyano-7-ethoxy-quinolin-6-yl) - acetamide (3) are used as raw material to prepare n- [4- [3- chloro-4- (pyridin-2-yl-methoxy) anilino] -3-cyano-7-ethoxy-quinolin-6-yl] acetamide (4) by nucleophilic substitution. deprotection of 4 was under the effect of hydrochloric acid, then was precipitated the free base in methanol solution of potassium carbonate to prepare 6-amino-3-cyano-4- [3-chloro-4- (pyridin-2-yl-methoxy) anilino] -7-ethoxy-quinoline (5). neratinib(1) was obtained by condensation of 5 and acyl chloride which was prepared by trans-4-dimethylamino-crotonic acid hydrochloride (6). figure 1 synthesis pathways of neratinib |
side effect | diarrhea, nausea, vomiting, and fatigue. |
usage | neratinib (hki-272) is a highly selective her2 and egfr inhibitor with ic50 of 59 nm and 92 nm, respectively. |
usage | an oral, irreversible dual egfr/her2 inhibitor for breast and non-small cell lung cancer. antitumor agent |
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