sapacitabine

Sapacitabine (CS682) is an orally available nucleoside analog precursor compound with potential anti-tumor activity for the study of acute myeloid leukemia.

CNDAC hydrochloride, a nucleoside analog, is a metabolite of the sapacitabine.

CNDAC, a nucleoside analog, is a major metabolite of oral drug sapacitabine.

RKS262 is a specific cyclin CDK 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.