ChemicalBook > Product Catalog > Biochemical Engineering > Inhibitors > protein tyrosine kinase > AZD-9291
AZD-9291 Chemical Properties
- Density 1.19±0.1 g/cm3(Predicted)
- CAS DataBase Reference1421373-65-0
- HS Code 29339900
AZD-9291 Usage And Synthesis
- UsesAZD-9291 (Osimertinib) is a oral, third generation, small-molecule epidermal growth factor receptor (EGFR) inhibitor and antineoplastic agent. In addition, it is a Cytochrome P450 3A inhibitor, and Cytochrome P450 3A4 Inducer, and Cytochrome P450 1A2 Inducer, and Breast Cancer Resistance Protein Inhibitor. It is used for the treatment of advanced non-small cell lung cancer (NSCLC) where mutant EGFR form (such as T790M) is often presented. Through suppressing the EGFR-mediated signalling, it cause cell death and inhibit tumour growth in related cancer cells.
- DescriptionAZD-9291 (Mesylate), also known as Osimertinib, belongs to a third-generation EGFR (epidermal growth factor receptor) inhibitor. It can be used for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) in case when the cancer cells carry specific mutations (such as T790M) in the epidermal growth factor receptor. It takes effect through directly binding to the certain mutant forms of EGFR (T790M, L858R, and exon 19 deletions) that are frequently found in NSCLC, further causing poor prognosis for late-stage disease. Since it spares wild type EGFR during therapy, it has only limited toxicity.
- UsesAZD 9291 is an irreversible inhibitor of epidermal growth factor receptor (EGFR) sensitizing and T790M resistance mutations (IC50s = 15-17 nM) while sparing the wild-type form of the receptor (IC50 = 480 nM). It binds the related IGF1R and hERG receptors with significantly reduced potency (IC50s = 2.9 and 16.2 μM, respectively). AZD 9291 has been shown to inhibit tumor growth in a xenograft mouse model at oral doses of 5-10 mg/kg and has been tested clinically in patients with advanced EGFR mutant non-small-cell lung cancer.[Cayman Chemical]
- DefinitionChEBI: A member of the class of aminopyrimidines that is 4-(1-methylindol-3-yl)pyrimidin-2-amine in which one of the amino hydrogens is replaced by a 2-methoxy-4-[2-(dimethylamino)ethyl](methyl)amino-5-acrylamidophenyl group. Used (as the mesylate salt) for treat ent of EGFR T790M mutation positive non-small cell lung cancer.
- IndicationsThe collection of ibrutinib (Imbruvica(R), Pharmacyclics Inc.), afatinib, and osimertinib represents the small, yet expanding, group of covalent SMKIs. Ibrutinib is a non-receptor Bruton’s tyrosine kinase inhibitor approved for the treatment of relapsed chronic lymphocytic leukemia. Afatinib, approved for NSCLC in 2013 and squamous NSCLC in 2016, is a second-generation irreversible EGFR inhibitor that targets wild-type EGFR, the mutant T790M EGFR, and HER2. Osimertinib (AZD9291), which was approved by FDA in November 2015, is a third-generation irreversible EGFR inhibitor that selectively targets the mutant T790M EGFR. Rociletinib, which shares a high degree of structural similarity with that of osimertinib, is a promising covalent EGFR inhibitor developed by Clovis Oncology aimed for the treatment of patients with EGFR T790M-mutated NSCLC, until the company terminated its development in May 2016 following a negative vote fromthe FDA’sOncologic Drugs Advisory Committee.
- Company Name:Nanjing Gold Pharmaceutical Technology Co. Ltd. Gold
- Company Name:Shanghai BLT Biological Pharmaceutical Co., Ltd. Gold
- Tel:021-20786057 18918495077
- Company Name:Jiangsu Vanadium Medicine Technology Co., Ltd. Gold
- Company Name:Zhejiang zetian fine chemical co. LTD Gold
- Company Name:Hubei Junxian Biotechnology Co., Ltd Gold