Biological Activity |
Oxaliplatin is a DNA synthesis inhibitor. It causes DNA crosslinking damage, prevents DNA replication and transcription and causes cell death. In Vitro: Oxaliplatin acts through the formation of DNA-adducts. Oxaliplatin induces primary and secondary DNA lesions leading to cell apoptosis[1]. Oxaliplatin inhibits human melanoma cell lines C32 and G361 with IC50 values of 0.98 mM and 0.14 mM, respectively[2]. Oxaliplatin potently inhibits bladder carcinoma cell lines RT4 and TCCSUP, ovarian carcinoma cell line A2780, colon carcinoma cell line HT-29, glioblastoma cell lines U-373MG and U-87MG, and melanoma cell lines SK-MEL-2 and HT-144 with IC50 of 11 uM, 15 uM, 0.17 uM, 0.97 uM, 2.95 uM, 17.6 uM, 30.9 uM and 7.85 uM, respectively[3]. In Vivo: Oxaliplatin (10 mg/kg, i.p.) significantly reduces tumor volume and apoptotic index in the nude mice bearing hepatocellular HCCLM3 tumors[4]. Oxaliplatin (5 mg/kg, i.v.) is effective on T-leukemia-lymphoma L40 AKR with T/C of 1.77. Oxaliplatin is efficient on intracerebrally grafted L1210 leukemia, MA 16-C xenografts, B16 melanoma xenografts, Lewis lung xenografts and C26 colon carcinoma xenografts[5]. Oxaliplatin induces impairment of retrograde neuronal transport in mice[6]. |