| Description | Namitecan is an effective inhibitor of topoisomerase I. It has antitumor property. |
| In vitro | Namitecan decreases a dose-dependent decrease in EGFR expression in the different cell lines[1]. Namitecan and cetuximab cooperate in inhibiting EGFR expression. ST1968 causes a comparable level of apoptosis in A431 and A431/TPT cells (IC50: 0.21 and 0.29 μM)[2]. |
| In vivo | Namitecan (10 mg/kg) in combination with cetuximab (1 mg/mouse) induces synergistic antitumor effects in SCC models as a function of EGFR gene copy number[1]. ST1968 (25 mg/kg) causes acceptable body weight loss and no toxic deaths. ST1968 produces a 100% complete response rate in the mice bearing the A431 tumor and retains a relevant activity in the topotecan-resistant tumor[2]. |
| Synonyms | ST-1968 |
| molecular weight | 434.44 |
| Molecular formula | C23H22N4O5 |
| CAS | 372105-27-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| References | 1. De Cesare M, et al. Synergistic antitumor activity of cetuximab and namitecan in human squamous cell carcinoma models relies on cooperative inhibition of EGFR expression and depends on high EGFR gene copy number. Clin Cancer Res. 2014 Feb 15;20(4):995-1006. 2. Zuco V, et al. Efficacy of ST1968 (namitecan) on a topotecan-resistant squamous cell carcinoma. Biochem Pharmacol. 2010 Feb 15;79(4):535-41. |