Product Name
Topotecan Hydrochloride
Synonyms
SKF 104864A Hydrochloride; NSC 609669 Hydrochloride
Description
Topotecan Hydrochloride (SKF 104864A Hydrochloride) is a Topoisomerase I inhibitor with potent antineoplastic activities.
Structural Formula
Topotecan Hydrochloride
Solubility
DMSO : 100 mg/mL(218.38 mM;Need ultrasonic) H2O : 33.33 mg/mL(72.79 mM;Need ultrasonic)
Source
Plants >Nyssaceae > Camptotheca acuminataDecne.
Storage
4℃, sealed storage, away from moisture and light
IC50 & Target
β adrenergic receptor
Shipping
Room temperature in continental US; may vary elsewhere.
SMILES
[H]Cl.O=C1[C@](O)(CC)C2=C(CO1)C(N3CC4=CC5=C(CN(C)C)C(O)=CC=C5N=C4C3=C2)=O
In Vivo
NUB-7 metastatic model, the animals belonging to all the 4 groups are sacrificed after 14 days of treatment. Compared with the control, Low dose metronomic (LDM) Topotecan Hydrochloride 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 Topotecan Hydrochloride+PZ to control liver metastasis. In a previous dose-response study, the daily dose of oral metronomic Topotecan Hydrochloride (0.5, 1.0, and 1.5 mg/kg) causes greater reduction in microvascular density compared with weekly maximum-tolerated dose regimen (7.5 and 15 mg/kg) in an ovarian cancer model, but the mice treated with 1.5 mg/kg daily, oral Topotecan Hydrochloride show decreased food intake, and a lesser antitumor effect.
In Vitro
Topotecan Hydrochloride (SKF 104864A Hydrochloride) obviously inhibits the proliferation of not only human glioma cells but also glioma stem cells (GSCs) in a dose- and time-dependent manner. According to the IC50 values at 24 h, 3 μM of Topotecan Hydrochloride is selected as the optimal administration concentration. In addition, Topotecan Hydrochloride induces cell cycle arrest in G0/G1 and S phases and promoted apoptosis. Results show that cell viability is inhibited by Topotecan Hydrochloride in a dose-dependent manner. 2, 20 and 40 μM of Topotecan Hydrochloride obviously inhibits the cell viability compared with the control groups. The IC50 values of Topotecan Hydrochloride at 24 h are 2.73±0.25 μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and 5.95±0.24 μM of GSCs-U87. Thus 3 μM of Topotecan Hydrochloride is selected as the optimal administration concentration in the subsequent experiments.
Datasheet 
