Aprinocarsen sodium (C09-1101-887)

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 VitroAprinocarsen 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 VivoAprinocarsen 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. Molecular Formula: C196H230N68Na19O105P19S19 Molecular Weight: 6852.85 PubChem CID: 71587700 Isomeric SMILES: CC1=CN(C(=O)NC1=O)[C@H]2C[C@@H]([C@H](O2)COP(=S)([O-])O[C@H]3C[C@@H](O[C@@H]3CO)N4C=NC5=C4N=C(NC5=O)N)OP(=S)([O-])OC[C@@H]6[C@H](C[C@@H](O6)N7C=C(C(=O)NC7=O)C)OP(=S)([O-])OC[C@@H]8[C@H](C[C@@H](O8)N9C=CC(=NC9=O)N)OP(=S)([O-])OC[C@@H]1[C@H](C[C@@H](O1)N1C=C(C(=O)NC1=O)C)OP(=S)([O-])OC[C@@H]1[C@H](C[C@@H](O1)N1C=CC(=NC1=O)N)OP(=S)([O-])OC[C@@H]1[C@H](C[C@@H](O1)N1C=NC2=C1N=C(NC2=O)N)OP(=S)([O-])OC[C@@H]1[C@H](C[C@@H](O1)N1C=CC(=NC1=O)N)OP(=S)([O-])OC[C@@H]1[C@H](C[C@@H](O1)N1C=C(C(=O)NC1=O)C)OP(=S)([O-])OC[C@@H]1[C@H](C[C@@H](O1)N1C=NC2=C1N=C(NC2=O)N)OP(=S)([O-])OC[C@@H]1[C@H](C[C@@H](O1)N1C=NC2=C1N=C(NC2=O)N)OP(=S)([O-])OC[C@@H]1[C@H](C[C@@H](O1)N1C=C(C(=O)NC1=O)C)OP(=S)([O-])OC[C@@H]1[C@H](C[C@@H](O1)N1C=NC2=C1N=C(NC2=O)N)OP(=S)([O-])OC[C@@H]1[C@H](C[C@@H](O1)N1C=NC2=C(N=CN=C21)N)OP(=S)([O-])OC[C@@H]1[C@H](C[C@@H](O1)N1C=NC2=C1N=C(NC2=O)N)OP(=S)([O-])OC[C@@H]1[C@H](C[C@@H](O1)N1C=C(C(=O)NC1=O)C)OP(=S)([O-])OC[C@@H]1[C@H](C[C@@H](O1)N1C=C(C(=O)NC1=O)C)OP(=S)([O-])OC[C@@H]1[C@H](C[C@@H](O1)N1C=C(C(=O)NC1=O)C)OP(=S)([O-])OC[C@@H]1[C@H](C[C@@H](O1)N1C=CC(=NC1=O)N)OP(=S)([O-])OC[C@@H]1[C@H](C[C@@H](O1)N1C=NC2=C(N=CN=C21)N)O.[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+]