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RKS262 is a specific cycliCDK inhibitor. RKS262 was identified by structural optimization of Nifurtimox which is currently undergoing phase II clinical trials to treat high-risk neuroblastoma. In a NCI(60) cell-line assay RKS262 exhibited significant cytotoxicity in ovarian cancer cells and a variety of other cell lines exceeding effects of commercial drugs such as cisplatin, 5-FU, cyclophosphamide or sapacitabine. Various leukemia cell-lines were most sensitive (GI(50):?~?10 nM) while several non-small cell lung cancer cell lines and few cell lines from other tissues were relatively resistant (GI(50)?>?1?μM) to RKS262 treatment. |
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