"目录号: HY-14821

Cell Cycle/DNA Damage-

Namitecan 是一种topoisomerase I抑制剂，具有抗肿瘤活性。

Topoisomerase

相关产品

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生物活性

Description

Namitecan is a potenttopoisomerase Iinhibitor, with antitumor property.

In Vitro

Namitecan and cetuximab cooperate in inhibiting EGFR expression. Namitecan induces a dose-dependent decrease in EGFR expression in the different cell lines[1]. ST1968 induces a comparable level of apoptosis in A431 and A431/TPT cells with IC50of 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].

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.