Topotecan

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

拓扑替康是一种拓扑异构酶 I 抑制剂，是一种用于治疗卵巢癌的抗肿瘤化合物，通过抑制 DNA 拓扑异构酶发挥作用。

Topotecan is a Topoisomerase I inhibitorand is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases.

Topotecan obviously inhibits proliferation of human glioma cells and glioma stem cells (GSCs) in a dose- and time-dependent manner. Topotecan (0-40 μM) obviously inhibits the cell viability compared with the control groups, in a dose-dependent manner.Topotecan shows anti-proliferation activity against U251, U87, GSCs-U251 and GSCs-U87 cells, with IC50 values of 2.73±0.25, 2.95±0.23, 5.46±0.41, and 5.95±0.24 μM, respectively.

NUB-7 metastatic model, the animals belonging to all the 4 groups are sacrificed after 14 days treatment. Compared with the control, Low dose metronomic (LDM) Topotecan (TP) and TP+Pazopanib (PZ) liver weights are significantly lower in TP+PZ-treated animals, compared with PZ. Microscopic tumors are visible in the livers of mice belonging to all the groups except TP+PZ confirming the ability of TP+PZ to control liver metastasis. Topotecan (0.5, 1.0, and 1.5 mg/kg; Orally, daily) causes greater reduction in microvascular density in an ovarian cancer model, but the mice treated with 1.5 mg/kg daily, oral Topotecan show decreased food intake, and a lesser antitumor effect.

SKF 104864A | NSC 609669

Cell Cycle/DNA Damage

Topoisomerase

Eukaryotic topoisomerase I

Cancer

small cell lung Cancer cervical Cancer

123948-87-8

421.45

C23H23N3O5

>98% (HPLC)

DMSO:84 mg/mL (199.31 mM)

CC[C@@]1(O)C(=O)OCc2c1cc1-c3nc4ccc(O)c(CN(C)C)c4cc3Cn1c2=O

——

(-20℃)

With Ice Pack

≥ 2 years