Aprinocarsen sodium

Aprinocarsen (ISIS 3521) sodium, a specific antisense oligonucleotide inhibitor of protein kinase C-alpha ( PKC-α ). Aprinocarsen sodium is a 20-mer oligonucleotide, it regulates cell differentiation and proliferation. Aprinocarsen sodium inhibits the growth of human tumor cell lines in nude mice. Aprinocarsen sodium shows the value as a chemotherapeutic compound of human cancers. In Vitro Aprinocarsen sodium dose-dependently and oligonucleotide sequence specifically inhibits PKC-alpha in human bladder carcinoma (T-24) cells. Aprinocarsen sodium shows an IC 50 value of 50-100 nM for PKC-α mRNA reduction, but it shows no effect on the expression of other members of the PKC family of genes (PKC-eta and zeta). MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Aprinocarsen sodium (100 mg/kg; i.v.; at repeat doses for 14 days) shows well tolerated character with no apparently acute toxicity . Aprinocarsen sodium (i.v.) dose-dependently inhibits the growth of T-24 bladder, human lung carcinoma (A549) and Colo 205 colon carcinoma human tumor cell lines in nude mice with ID 50 values of 0.06-0.6 mg/kg daily . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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