An orally available antineoplastic platinum(IV) complex
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Satraplatin is an orally available antineoplastic platinum(IV) complex.1 It is more hydrophobic than cisplatin or oxaliplatin , which reduces transport-determined acquired resistance.1 Satraplatin also displays less neurotoxicity in rats than cisplatin or tetraplatin.2 Satraplatin has a favorable toxicity profile and appears to have clinical activity against a variety of malignancies.3
1.Kelland, L.R., Abel, G., McKeage, M.J., et al.Preclinical antitumor evaluation of bis-acetato-ammine-dichloro-cyclohexylamine platinum(IV): An orally active platinum drugCancer Res.53(11)2581-2586(1993) 2.McKeage, M.J., Boxall, F.E., Jones, M., et al.Lack of neurotoxicity of oral bisacetatoamminedichlorocyclohexylamine-platinum(IV) in comparison to cisplatin and tetraplatin in the ratCancer Res.54(3)629-631(1994) 3.Bhargava, A., and Vaishampayan, U.N.Satraplatin: Leading the new generation of oral platinum agentsExpert. Opin. Investig. Drugs18(11)1787-1797(2009)
Cell experiment: | Cells are harvested, counted and distributed to microtiter plates in 100 μL medium at a density of 1×104 cells/well. Appropriate dilutions of test compounds (Satraplatin, etc.) are added to a total volume of 200 μL/well and plates incubated under tissue culture conditions for four days. Stock solutions of the compounds are prepared in either 70% ethanol or DMSO and diluted more than 100-fold for the assays. Solvent controls are included in all tests. Dose response curves are obtained by assessing cell proliferation at twofold drug dilutions in triplicate and used for calculation of IC50 values. Cell growth is quantified using a modified tetrazolium dye assay (MTT) and by measurement of the reduced formazane dye at 450 nm wavelength (medium control set to 100% proliferation)[1]. |
参考文献: [1]. Fiebiger W, et al. In vitro cytotoxicity of novel platinum-based drugs and dichloroacetate against lung carcinoid cell lines. Clin Transl Oncol. 2011 Jan;13(1):43-9. |
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