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[1].
Aprinocarsen sodium dose-dependently and oligonucleotide sequence specifically inhibits PKC-alpha in human bladder carcinoma (T-24) cells[1].
Aprinocarsen sodium shows an IC50 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)[1].
Aprinocarsen sodium (100 mg/kg; i.v.; at repeat doses for 14 days) shows well tolerated character with no apparently acute toxicity[1].
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 ID50 values of 0.06-0.6 mg/kg daily[1].
[1]. https://pubmed.ncbi.nlm.nih.gov/8758918/