755. Aprinocarsen

Nomenclature

CAS number: 151879-73-1
d(P-Thio)(G-T-T-C-T-C-G-C-T-G-G-T-G-A-G-T-T-T-C-A)DNA; CGP-64128A; ISI-641A; LY-900003.
C196H249N68O105P19S19; mol wt 6435.20.
C 36.58%, H 3.90%, N 14.80%, O 26.11%, P 9.15%, S 9.47%.

Description and references

Synthetic, 20 base phosphorothioate antisense oligonucleotide designed to inhibit protein kinase C-α (PKC-α) expression. Prepn: C. F. Bennett, N. Dean, WO 9319203; eidem, US 5882927 (1993, 1999 both to Isis). Pharmacology: N. Dean et al., Cancer Res. 56, 3499 (1996). CGE determn in tissue: R. S. Geary et al., Anal. Biochem. 274, 241 (1999). Clinical pharmacology and evaluation in advanced cancer: J. Nemunaitis et al., J. Clin. Oncol. 17, 3586 (1999). Review of pharmacokinetics: P. L. Nicklin et al., Handb. Exp. Pharmacol. 131, 141-168 (1998). Review of development and clinical evaluations: J. T. Holmlund et al., Curr. Opin. Mol. Ther. 3, 372-385 (1999); K. Li, J. Zhang, Curr. Opin. Investig. Drugs 2, 1454-1461 (2001).

Derivative

Nonadecasodium salt.

Nomenclature

CAS number: 331257-53-5
Aprinocarsen sodium; ISIS-3521; Affinitac (Lilly); Affinitak (Lilly).
C196H230N68Na19O105P19S19; mol wt 6852.86.
C 34.35%, H 3.38%, N 13.90%, Na 6.37%, O 24.51%, P 8.59%, S 8.89%.

Therapeutic Category

Antineoplastic.

Keywords

Antineoplastic; Oligonucleotides