Neratinib

Neratinib
Neratinib
Neratinib

Neratinib

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100 Gram

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  • Min.Order :100 Gram
  • Purity: 99%
  • Payment Terms : L/C,D/A,D/P,T/T,,MoneyGram,Other

Keywords

neratinib HIGH purity by own lab 698387-09-6 Unii-jjh94R3pwb

Quick Details

  • Appearance: white to brown low melting crystalline solid
  • Application: 698387-09-6 Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM, respectively.
  • PackAge:1g;5g;10g;25g;50g;100g;500g;1KG;5KG,25kg,50kg or as customers request
  • ProductionCapacity:100|Kilogram|Month
  • Storage:2-8, cold storage, to avoid light storage.
  • Transportation:BY SEA /BY AIR /BY COURIER

Superiority:

 
Neratinib Basic information
New anticancer drug Synthesis pathways Side effect
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 Structure
 
Neratinib Chemical Properties
density  1.33
 
Safety Information
MSDS 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). 
Synthesis pathways of Neratinib
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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