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SynKinase
Afatinib
CHF 0.00
In stock
SYN-1100-M0011 mgCHF 114.00
SYN-1100-M0055 mgCHF 170.00
SYN-1100-M01010 mgCHF 284.00
SYN-1100-M05050 mgCHF 780.00
SYN-1100-M100100 mgINQ
| Product Details | |
|---|---|
| Synonyms | Tovok; BIBW-2992 |
| Product Type | Chemical |
| Properties | |
| Formula | C24H25ClFN5O3 |
| MW | 486.0 |
| CAS | 439081-18-2 |
| Purity Chemicals | ≥95% |
| Appearance | Solid. |
| Solubility | Soluble in DMSO or ethanol. |
| Declaration | Manufactured by SynKinase. |
| Other Product Data |
Target: EGFR - HER2 | Kinase Group: RTK | Substrate: Tyrosine Click here for Original Manufacturer Product Datasheet Our product description may differ slightly from the original manufacturers product datasheet. |
| InChi Key | ULXXDDBFHOBEHA-CWDCEQMOSA-N |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
Afatinib is an irreversible kinase inhibitor and binds to the kinase domains of EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4) to inhibit tyrosine kinase autophosphorylation. This results in a downregulation of ErbB signaling and subsequent inhibition of proliferation of cell lines expressing wild-type EGFR, selected EGFR exon 19 deletion mutations, or exon 21 L858R mutations. It also inhibited in vitro proliferation of cell lines overexpressing HER2. Overall, tumor growth was inhibited by Afatinib very effectively with low nanomolar IC(50) values ranging from approximately 6nM to below 500nM.
Product References
- Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors: K.L. Stevens, et al.; Bioorg. Med. Chem. Lett. 19, 21 (2009)
- Irreversible protein kinase inhibitors: balancing the benefits and risks: T. Barf & A. Kaptein; J. Med. Chem. 55, 6243 (2012)
- Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR): R.A. Ward, et al.; J. Med. Chem. 56, 7025 (2013)
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