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CAS RN: 850140-72-6 | Product Number: A2870
Afatinib
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Purity: >97.0%(HPLC)(N)
Synonyms:
Product Documents:
| Size | Unit Price | Belgium | Japan* |
|---|---|---|---|
| 50MG |
€53.00
|
1 | ≥40 |
| 250MG |
€168.00
|
1 | 24 |
*Stock available in Belgium will be delivered in 1 to 3 days
*Stock available in Japan will be delivered in 1 to 2 weeks (excludes regulated items and dry ice shipments).
| Product Number | A2870 |
| Purity / Analysis Method | >97.0%(HPLC)(N) |
| Molecular Formula / Molecular Weight | C__2__4H__2__5ClFN__5O__3 = 485.94 |
| Physical State (20 deg.C) | Solid |
| Storage Temperature | Refrigerated (0-10°C) |
| Condition to Avoid | Heat Sensitive |
| CAS RN | 850140-72-6 |
| Reaxys Registry Number | 11746023 |
| PubChem Substance ID | 468590121 |
| MDL Number | MFCD12407405 |
Specifications
| Appearance | White to Orange to Green powder to crystal |
| Purity(HPLC) | min. 97.0 area% |
| Purity(with Total Nitrogen) | min. 97.0 % |
| Water | max. 3.0 % |
| NMR | confirm to structure |
Properties (reference)
| Melting Point | 102 °C |
GHS
Related Laws:
Transport Information:
| HS Number | 2934999090 |
Application
Afatinib: An Irreversible Inhibitor of the ErbB Family of Tyrosine Kinases
Afatinib (BIBW-2992) is an irreversible inhibitor of the ErbB family of tyrosine kinases. The ErbB receptor tyrosine kinase family consists of four cell surface receptors: ErbB1/EGFR/HER1, ErbB2/HER2, ErbB3/HER3, and ErbB4/HER4. Deregulation of the ErbB receptor network is well recognized as an oncogenic driver in epithelial cancers. Afatinib downregulates ErbB signaling by covalently binding through a Michael addition reaction to the kinase domains of ErbB1/EGFR/HER1, ErbB2/HER2 and ErbB4/HER4, irreversibly inhibiting tyrosine kinase autophosphorylation. Afatinib was approved by FDA for the treatment of EGFR mutated non-small cell lung cancer in 2013. (The product is for research purpose only.)
References
- 1) BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models
- 2) Target binding properties and cellular activity of afatinib (BIBW 2992), an irreversible ErbB family blocker
- 3) Afatinib: First Global Approval (a review)
- 4) A comprehensive review of the preclinical efficacy profile of the ErbB family blocker afatinib in cancer
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