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SynKinase
Pelitinib
CHF 0.00
In stock
SYN-1141-M0011 mgCHF 114.00
SYN-1141-M0055 mgCHF 170.00
SYN-1141-M01010 mgCHF 298.00
SYN-1141-M05050 mgCHF 1'015.00
SYN-1141-M100100 mgINQ
| Product Details | |
|---|---|
| Synonyms | EKB-569 |
| Product Type | Chemical |
| Properties | |
| Formula | C24H23ClFN5O2 |
| MW | 467.9 |
| CAS | 257933-82-7 |
| 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 | WVUNYSQLFKLYNI-AATRIKPKSA-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
Pelitinib, also known as EKB 569, is a potent, irreversible inhibitor of the EGFR tyrosine kinase. Cell based IC(50) values range from 39nM to 80nM and in vitro kinase assays are in sub-nanomolar range for EGFR receptors. In xenograft tumor models using overexpressing A431 cells Pelitinib inhibits growth of tumors with effective doses of 3.5-10mg/kg/dl. Recent research also shows that Pelitinib can potentiate radiation induced killing of squamouse cell carcinoma via the inhibition of IR-induced NF-κB mediated cell survial pathway.
Product References
- Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2: A. Wissner, et al.; Bioorg. Med. Chem. 15, 3635 (2007)
- A quantitative analysis of kinase inhibitor selectivity: M.W. Karaman, et al.; Nat. Biotechnol. 26, 127 (2008)
- Development of a new epidermal growth factor receptor positron emission tomography imaging agent based on the 3-cyanoquinoline core: synthesis and biological evaluation: F. Pisaneschi, et al.; Bioorg. Med. Chem. 18, 6634 (2010)
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