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Neratinib Suppliers list
Company Name:Jiangsu Allyrise Pharmaceutical Co., LTD  Gold
Tel:+86-523-86818697 18652728585
Company Name:Longdo (Shanghai) Biotechnology Co., Ltd.  Gold
Company Name:SPIRO PHARMA  Gold
Company Name:Hefei NaNo Biological Technology Co., Ltd.  Gold
Company Name:Suzhou Shang Enda Biotechnology Ltd.  Gold
Tel:0512-66907022 18036087221
Neratinib Basic information
New anticancer drug Synthesis pathways Side effect
Product Name:Neratinib
Product Categories:Antineoplastic;Anti-cancer & immunity;Inhibitors
Mol File:698387-09-6.mol
Neratinib Structure
Neratinib Chemical Properties
density 1.33
Safety Information
MSDS Information
Neratinib Usage And Synthesis
New anticancer drugNeratinib 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 pathways3-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).
Synthesis pathways of Neratinib
Figure 1 Synthesis pathways of Neratinib
Side effectDiarrhea, nausea, vomiting, and fatigue.
UsageNeratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM, respectively.
UsageAn oral, irreversible dual EGFR/HER2 inhibitor for breast and non-small cell lung cancer. Antitumor agent
Neratinib Preparation Products And Raw materials
Tag:Neratinib(698387-09-6) Related Product Information
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