| Description | CT-2584 is an anticancer agent that inhibits phospholipid signaling and kills tumor cells through the production of reactive oxygen intermediates. CT-2584 reduces NKEF-B expression in several tumor cell types.CT-2584 reduced tumor growth in SCID mice by causing shunting of ab initio phospholipid biosynthesis from phosphatidylcholine (PC) to phosphatidylinositol (PI) via PA. |
| In vitro | CT-2584 （0-7 μM，3 天）对 ECV304 有毒性，而 B/1 细胞对其有很强的抗性。[5]；人类肝细胞癌Alex 0细胞在3.5 mmol/L的CT-2584下，Alex 0.5细胞在2.0 mmol/L的CT-2584下观察到毒性。24小时后，即使在更低的浓度下，也观察到了细胞毒性和HBsAg（乙型肝炎表面抗原）分泌的减少。[6] |
| In vivo | 每天腹腔注射25 mg/kg CT-2584连续三天对SCID小鼠是可耐受的。尝试更高剂量（50 mg/kg）时，因药物相关的腹膜炎导致动物死亡。[6] |
| Synonyms | CT2584, CT 2584 |
| molecular weight | 533.79 |
| Molecular formula | C30H55N5O3 |
| CAS | 166981-13-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Bonfil RD,et al. CT-2584 (Cell Therapeutics). Curr Opin Investig Drugs. 2001 Mar;2(3):424-7. 2. Cheeseman SL, et al. Phase I and pharmacologic study of CT-2584 HMS, a modulator of phosphatidic acid, in adult patients with solid tumours. Br J Cancer. 2000 Dec;83(12):1599-606. 3. Finney RE, et al.Pharmacological inhibition of phosphatidylcholine biosynthesis is associated with induction of phosphatidylinositol accumulation and cytolysis of neoplastic cell lines. Cancer Res. 2000 Sep 15;60(18):5204-13. 4. Khan P, et al.Development and validation of a sensitive solid-phase extraction and high-performance liquid chromatography assay for the novel antitumour agent CT2584 in human plasma. J Chromatogr B Biomed Sci Appl. 1999 Jan 22;721(2):279-84. 5. Shau H,et al. Endogenous natural killer enhancing factor-B increases cellular resistance to oxidative stresses. Free Radic Biol Med. 1997;22(3):497-507. 6. Marucci L,et al. Effect of a xanthine analog on human hepatocellular carcinoma cells (Alexander) in culture and in xenografts in SCID mice. Hepatology. 1997 Nov;26(5):1195-202. |