ChemicalBook > Product Catalog >API >Antineoplastic agents >Tinib Antineoplastic drugs >Neratinib

Neratinib

Neratinib Suppliers list
Company Name: Shanghai Jinghao Pharmaceutical Co.,Ltd
Tel: +86-21-68900963
Email: sales@jinghaopharma.com
Products Intro: Product Name:Neratinib
CAS:698387-09-6
Purity:99.5% Package:1kg 25kg per barrel Remarks:pharmaceutical intermediates;
Company Name: Jurong Coupling Biotechnology Co., Ltd.
Tel: 13656108824
Email: coupling278191416@hotmail.com
Products Intro: Product Name:Neratinib
CAS:698387-09-6
Purity:99% HPLC Package:5KG;1KG
Company Name: Capot Chemical Co.,Ltd.
Tel: +86-571-85586718
Email: sales@capotchem.com
Products Intro: Product Name:Neratinib(HKI-272)
CAS:698387-09-6
Purity:98%(Min,HPLC) Package:100g;1kg;5kg,10kg,25kg,50kg
Company Name: Henan DaKen Chemical CO.,LTD.
Tel: +86-371-55531817
Email: info@dakenchem.com
Products Intro: Product Name:Neratinib
CAS:698387-09-6
Purity:99% Package:100g,500g,1kg,5kg,10kg
Company Name: Beijing Cooperate Pharmaceutical Co.,Ltd
Tel: 010-60279497
Email: sales01@cooperate-pharm.com
Products Intro: Product Name:Neratinib
CAS:698387-09-6
Purity:99% Package:1G;50USD

Lastest Price from Neratinib manufacturers

  • Neratinib
  • US $7.00 / KG
  • 2019-07-06
  • CAS: 698387-09-6
  • Min. Order: 1KG
  • Purity: 99%
  • Supply Ability: 1000KG
  • Neratinib
  • US $100.00 / KG
  • 2019-07-06
  • CAS:698387-09-6
  • Min. Order: 1KG
  • Purity: 98%
  • Supply Ability: 100KG

Related articles

  • Neratinib- pharmacology
  • Neratinib is an oral pan HER inhibitor that irreversibly inhibits the tyrosine kinase activity of epidermal growth factor rece....
  • Dec 13,2019
Neratinib Basic information
New anticancer drug Genotoxicity Clinical trial Synthesis pathways Side Effects
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(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;HKI-272; HKI272; HKI 272
CAS:698387-09-6
MF:C30H29ClN6O3
MW:557.04266
EINECS:811-237-1
Product Categories:Inhibitors;Anti-cancer & immunity;Antineoplastic;API
Mol File:698387-09-6.mol
Neratinib Structure
Neratinib Chemical Properties
Boiling point 757.0±60.0 °C(Predicted)
density 1.33
form Off-white solid.
pka12.37±0.43(Predicted)
Safety Information
HS Code 29334900
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.
Genotoxicity

Neratinib and its metabolites were not genotoxic. Administration of neratinib to pregnant rabbits during organogenesis resulted in abortions, embryo-fetal death, and fetal abnormalities at maternal exposures (AUC) approximately 0.2 times exposures in patients at the recommended dose. Oral administration of neratinib to pregnant rats from gestation day 7 until lactation day 20 resulted in effects on long-term memory in male offspring at maternal doses less than the maximum recommended clinical dose on a mg/m2 basis. Neratinib was not carcinogenic in a 26-week carcinogenicity study in rasH2 transgenic mice.

Clinical trial

Neratinib was tested in a phase II trial as monotherapy in 2 cohorts of patients with advanced HER2-positive breast cancer those with and those without previous trastuzumab treatment. Sixteen-week progression-free survival (PFS) rates were 59% for patients with previous trastuzumab treatment and 78% for patients with no previous trastuzumab treatment with a median PFS of 22.3 and 39.6 weeks, respectively. Objective response rates were 24% among patients with previous trastuzumab treatment and 56% in the trastuzumab-naive cohort.[4]

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 EffectsDiarrhea, nausea, vomiting, and fatigue.
UsesNeratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM, respectively.
UsesAn oral, irreversible dual EGFR/HER2 inhibitor for breast and non-small cell lung cancer. Antitumor agent
DefinitionChEBI: 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.
Neratinib Preparation Products And Raw materials
Tag:Neratinib(698387-09-6) Related Product Information
AKOS B033273 AZD-9291 n-(4-Chloro-3-cyano-7-ethoxy-6-quinolinyl) acetamide 6-amino-4-(3-chloro-4-(pyridin-2-ylmethoxy)phenylamino)-7-ethoxyquinoline-3-carbonitrile Lenvatinib Tofacitinib Axitinib Paclitaxel Gefitinib Bortezomib ABT 263 Ibrutinib Crizotinib Afatinib Lapatinib Ditosylate Ethoxyquin 4-(pyridin-2-ylmethoxy)aniline Neratinib