Oxaliplatin (CAS: 61825-94-3)

C₈H₁₄N₂O₄Pt

• Potent platinum-based antineoplastic agent with wide spectrum anticancer activity [2, 7-9].
• Anticancer compound. Forms inter- and intrastrand DNA adducts/crosslinks, consequently blocking DNA replication and transcription and inducing cell death [1, 4, 7, 10, 13].
• Shows antitumor activity in cisplatin resistant cell lines [3, 8].
• Shows better biochemical, pharmacological and cytotoxic properties than cisplatin (Prod. No. AG-CR1-3590) and carboplatin (Prod. No. AG-CR1-3591) [5, 7, 8].
• Apoptosis inducer [10, 11].
• Targets other proteins and enzymes [6].
• Anticancer activity and antitumor specificity depends on selective uptake through human organic cation transporters 1 (OCT1) and OCT2 [12].
• Neurotoxic profile depends on organic cation transporter 2 (OCT2) uptake [14].

1. Cytotoxicity, cellular accumulation and DNA binding of oxaliplatin isomers: L. Pendyala, et al.; Cancer Lett. 97, 177 (1995)
2. Oxaliplatin: mechanism of action and antineoplastic activity: E. Raymond, et al.; Semin. Oncol. 25, 4 (1998) (Review)
3. Induction of JNK and c-Abl signalling by cisplatin and oxaliplatin in mismatch repair-proficient and -deficient cells: A Nehme, et al.; Br. J. Cancer 79, 1104 (1999)
4. Oxaliplatin-induced damage of cellular DNA: J.M. Woynarowski, et al.; Mol. Pharmacol. 58, 920 (2000)
5. What is the "best" platinum: cisplatin, carboplatin, or oxaliplatin? J. Lokich; Cancer Invest. 19, 756 (2001)
6. Biomolecular targets for platinum antitumor drugs: R.N. Bose; Mini Rev. Med. Chem. 2, 103 (2002)
7. Cellular and molecular aspects of drugs of the future: oxaliplatin: A.M. Di Francesco, et al.; Cell. Mol. Life Sci. 59, 1914 (2002) (Review)
8. Cellular and molecular pharmacology of oxaliplatin: E. Raymond, et al.; Mol. Cancer Ther. 1, 227 (2002)
9. New clues for platinum antitumor chemistry: Kinetically controlled metal binding to DNA: J. Reedijk; PNAS 100, 3611 (2003)
10. DNA strand breaks and apoptosis induced by oxaliplatin in cancer cells: S. Faivre, et al.; Biochem. Pharmacol. 66, 225 (2003)
11. Apoptosis induced by oxaliplatin in human colon cancer HCT15 cell line: P. Marchetti, et al.; Anticancer Res. 24, 219 (2004)
12. Organic cation transporters are determinants of oxaliplatin cytotoxicity: S. Zhang, ;et al.; Cancer Res. 66, 8847 (2006)
13. Inhibition of transcription by platinum antitumor compounds: R.C. Todd & S.J. Lippard; Metallomics 1, 280 (2009) (Review)
14. Oxaliplatin-induced neurotoxicity is dependent on the organic cation transporter OCT2: J.A. Sprowl, et al.; PNAS 110, 11199 (2013)