Pelitinib
Pelitinib is an irreversible EFGR inhibitor that exhibits anticancer chemotherapeutic benefit in the treatment of non-small cell lung cancer (NSCLC) and other solid tumor cancers. In vitro, pelitinib inhibits NF-κB, inhibiting transcription of TERT and telomerase activity. Pelitinib also decreases phosphorylation of Akt and ERK and induces cell cycle arrest in vitro.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18952803
| Cas No. |
257933-82-7 |
|---|---|
| Purity |
≥98% |
| Formula |
C24H23ClFN5O2 |
| Formula Wt. |
467.92 |
| Chemical Name |
(E)-N-(4-((3-chloro-4-fluorophenyl)amino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)but-2-enamide |
| IUPAC Name |
(E)-N-[4-(3-chloro-4-fluoroanilino)-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide |
| Synonym |
EKB-569 |
| Melting Point |
188-190°C (lit.) |
| Solubility |
Insoluble in water. Soulble in DMSO (≥13 mg/mL). |
| Appearance |
White Powder |
Aravindan N, Aravindan S, Herman TS, et al. EGFR tyrosine kinase inhibitor pelitinib regulates radiation-induced p65-dependent telomerase activation in squamous cell carcinoma. Radiat Res. 2013 Mar;179(3):304-12. PMID: 23379415.
Kim H, Lim HY. Novel EGFR-TK inhibitor EKB-569 inhibits hepatocellular carcinoma cell proliferation by AKT and MAPK pathways. J Korean Med Sci. 2011 Dec;26(12):1563-8. PMID: 22147992.
Yoshimura N, Kudoh S, Kimura T, et al. EKB-569, a new irreversible epidermal growth factor receptor tyrosine kinase inhibitor, with clinical activity in patients with non-small cell lung cancer with acquired resistance to gefitinib. Lung Cancer. 2006 Mar;51(3):363-8. PMID: 16364494.
