Title: Picoplatin
CAS Registry Number: 181630-15-9
CAS Name: (SP-4-3)-Amminedichloro(2-methylpyridine)platinum
Additional Names: cis-amminedichloro(2-methylpyridine)platinum(II)
Manufacturers' Codes: AMD-473; JM-473; NX-473; ZD-473
Molecular Formula: C6H10Cl2N2Pt
Molecular Weight: 376.15
Percent Composition: C 19.16%, H 2.68%, Cl 18.85%, N 7.45%, Pt 51.86%
Literature References: Third generation, sterically hindered Pt-complex that exhibits reduced reactivity with sulfur ligands such as glutathione, q.v.; designed to overcome acquired Pt-chemotherapy resistance. Prepn: B. A. Murrer, EP 727430 (1996 to AnorMED; Inst. of Cancer Research); idem, US 5665771 (1997 to Johnson Matthey). Pharmacology and pharmacokinetics: F. I. Raynaud et al., Clin. Cancer Res. 3, 2063 (1997). Cytotoxicity and DNA binding activity: J. Holford et al., Anti-Cancer Drug Design 13, 1 (1998). In vitro circumvention of cisplatin resistance: idem, et al,. Br. J. Cancer 77, 366 (1998); of radiosensitizing activity: G. P. Raaphorst et al., Anticancer Res. 24, 613 (2004). LC/MS determn in plasma: T. Oe et al., Anal. Chem. 74, 591 (2002); in urine: eidem, J. Chromatogr. B 792, 217 (2003). Series of articles on clinical evaluations: Eur. J. Cancer 38, Suppl. S1-S31 (2002). Review of early development: L. R. Kelland et al., J. Inorg. Biochem. 77, 111-115 (1999); and therapeutic potential: M. P. Hay, Curr. Opin. Invest. Drugs 1, 263-266 (2000).
Properties: Pale yellow solid. Sensitive to light. uv max (0.15M sodium chloride): 268 nm. A250/A268 = 0.62. LD50 in mice (mg/kg): 43 i.p., 560 orally (Murrer).
Absorption maximum: uv max (0.15M sodium chloride): 268 nm
Toxicity data: LD50 in mice (mg/kg): 43 i.p., 560 orally (Murrer)
Therap-Cat: Antineoplastic.
Keywords: Antineoplastic; Platinum Complexes. |