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- Chemical Name: Afatinib
- CAS No.: 850140-72-6
- Molecular Fomula: ： C24H25ClFN5O3
- Molecular weight： 485.94
- Appearance: Grayish white solid
- Sample：Available
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Description of 2-methanesulfonyl-ethylamine
Afatinib (INN; trade name Gilotrif in the US and Giotrif in Europe, previously Tomtovok and Tovok) is a drug approved in United States, Europe, Taiwan, Mexico, Chile and Japan as well as other countries for the first-line treatment of patients with distinct types of metastatic (EGFR mutation positive) non-small cell lung carcinoma (NSCLC), developed by Boehringer Ingelheim. It acts as an irreversible covalent inhibitor of the receptor tyrosine kinases epidermal growth factor receptor (EGFR) and erbB-2 (HER2).
Basic Info of 2-methanesulfonyl-ethylamine
Basic Info
Numbering system
Properties
Basic Info
| Chemical Name | 2-methanesulfonyl-ethylamine |
| Synonyms | BIBW 2992;2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-, (2E)-;(E)-Afatinib;Tovok;Afatinib freebase;Expand |
| CAS No. | 850140-72-6 |
| Molecular Formula | C24H25ClFN5O3 |
| Molecular Weight | 485.93800 |
| PSA | 88.61000 |
| LogP | 4.53590 |
Numbering system
| UNII | 41UD74L59M |
Properties
| Appearance & Physical State | Off-White Solid |
| Melting Point | 100 – 102 °C |
What is Afatinib?
- With the progress of science and technology and the development of society, chemical products have invariably permeated our daily lives, in medicine, food, cosmetics, electronics, industry, and other areas, becoming an essential part of our lives. One such product is Afatinib which has developed particularly rapidly in recent years. Do you know about Afatinib ?
- The official answer：Afatinib (afatinib) is a potent, irreversible dual inhibitor of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) tyrosine kinases. It is indicated for the treatment of 1 Locally advanced or metastatic non-small cell lung cancer (NSCLC) with an epidermal growth factor receptor (EGFR) sensitive mutation, not previously treated with an EGFR tyrosine kinase inhibitor (TKI) 2 Locally advanced or metastatic squamous histological type of non-small cell lung cancer (NSCLC) with disease progression during or after platinum-containing chemotherapy
What’s the application of Afatinib?
- Afatinib is an irreversible ErbB family blocker that inhibits messaging and blocks the major channels associated with cancer cell growth and division. Since the mechanism of information transmission through the ErbB family can be triggered by multiple homodimers and heterodimers, simultaneous inhibition of multiple ErbB family members (e.g., EGFR, HER2, ErbB3, and ErbB4) is more effective in interrupting downstream information transmission.
- In cancer cells, the operation of the ErbB family is often dysregulated. When factors that control cell growth mechanisms are over-expressed or function abnormally, there is a chance that various parenchymal solid tumors may develop. Over-expression of receptors stimulates intracellular information transmission beyond normal levels, resulting in uncontrolled tumor cell growth, migration and metastasis, and inhibition of apoptosis. These abnormalities in cellular information transmission can be caused by various mechanisms: receptor mutations (e.g. EGFR mutations in lung cancer tumors), receptor over-expression (e.g. HER2 overexpression in breast cancer tumors), or ligand over-expression.
Conclusion
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