166981-13-1

CT-2584 (166981-13-1; free base) is a cytotoxic agent that alters phospholipid biosynthesis via inhibition of CTP:choline-phosphate cytidylyltransferase causing an increase in phosphatidylinositol with decreasing levels of phosphatidylcholine.1?The altered phospholipid metabolism caused by CT-2584 results in a loss of lamellar structure and membrane integrity (especially in mitochondria and endoplasmic reticulum). CT-2584 was active against a wide range of tumor cell lines including multi-drug resistant lines.2

1) Finney?et al. (2000),?Pharmacological Inhibition of Phosphatidylcholine Biosynthesis is Associated with Induction of Phosphatidylinositol Accumulation and Cytolysis of Neoplastic Cell lines; Cancer Res.,?60?5204 2) Cheeseman?et al. (2000),?Phase I and pharmacologic study of CT-2584 HMS, a modulator of phosphatidic acid, in adult patients with solid tumors; Br. J. Cancer,?83?1599