Pelitinib specifically targets cancer cells with elevated expression of the efflux transporters ATP-binding cassette (ABC)B1/ABCG2 post hyperthermia. This property of peltinib aids in the elimination of metastasis and prevention of cancer recurrence.
Pelitinib (EKB-569) is an orally active, potent, second generation irreversible epidermal growth factor receptor tyrosine kinase (EGFR TK) inhibitor. Pelitinib is selective for EGFR (ErbB-1) with an IC50 about 80 nM, but also covalently binds to ErbB-2 (HER2/c-neu) and ErbB-4 (Her 4) with much lower potency. Pelitinib has been shown to inhibit the growth of EGFR-overexpressing tumor cell lines.
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Light sensitive
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