SKF 104864A; NSC 609669 MedChemExpress (MCE)

Product Name	Topotecan
Synonyms	hycamptamine Hycamptamine HYDROGEN CHLORIDE GAS HYDROCHLORIC ACID, 1N HYDROCHLORIC ACID,1.1M HYDROGEN CHLORIDE, BUTANOL REAGENT HYDROGEN CHLORIDE, METHANOL REAGENT Synonyms hycamptamine Hycamptamine HYDROGEN CHLORIDE GAS HYDROCHLORIC ACID, 1N HYDROCHLORIC ACID,1.1M HYDROGEN CHLORIDE, BUTANOL REAGENT HYDROGEN CHLORIDE, METHANOL REAGENT HYDROGEN CHLORIDE, METHANOL REAGENT 5 HYDROGEN CHLORIDE, METHANOL REAGENT 10 9-Dimethylaminomethyl-10-hydroxycamptothecin, HCl salt
CAS	123948-87-8
EINECS	687-471-1
Chemical Formula	C23H23N3O5
Molecular Weight	421.45
inchi	InChI=1/C23H23N3O5/c1-4-23(30)16-8-18-20-12(9-26(18)21(28)15(16)11-31-22(23)29)7-13-14(10-25(2)3)19(27)6-5-17(13)24-20/h5-8,27,30H,4,9-11H2,1-3H3
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Descriptions	Topotecan Topotecan MedChemExpress (MCE) HY-13768 123948-87-8 SKF 104864A Descriptions Topotecan Topotecan MedChemExpress (MCE) HY-13768 123948-87-8 SKF 104864A NSC 609669 Please store the product under the recommended conditions in the Certificate of Analysis. Room temperature in continental US may vary elsewhere. Topotecan (SKF 104864A NSC 609669) is an orally active and potent Topoisomerase I inhibitor. Topotecan induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan shows anticancer activity. Topotecan obviously inhibits proliferation of human glioma cells and glioma stem cells (GSCs) in a dose- and time-dependent manner[1]. Topotecan (0-40 μM) obviously inhibits the cell viability compared with the control groups, in a dose-dependent manner[1]. 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[1]. 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[2]. 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[2]. Mice[2] For subcutaneous xenograft studies, we used SK-N-BE, SH-SY5Y, KHOS, and RH30. 1×106 cells are implanted subcutaneously into the inguinal fat pad of each of nonobese diabetic/severe combined immune deficient (NOD/SCID) mice. When tumors reached 0.5 cm in diameter, the animals are randomized into 4 groups and treated daily by oral gavage. The animals are grouped as: Control group, LDM Topotecan group or LDM TP (1 mg/kg Topotecan), Pazopanib group or PZ (150 mg/kg Pazopanib) and combination group or TP+PZ (1 mg/kg Topotecan+150 mg/kg Pazopanib). To compare pulse Topotecan with LDM TP in KHOS osteosarcoma model, PZ is replaced by weekly oral dose of pulse Topotecan (SKF104864) or Pulse TP (15 mg/kg Topotecan (SKF104864)). The criteria for endpoint are tumor sizes exceeding 2.0 cm in diameter or animals showing signs of morbidity. The tumor sizes are measured on a daily basis until the endpoint or sacrifice. The long (D) and short diameters (d) are measured with calipers. Tumor volume (cm3) is calculated as V=0.5×D×d2. When the endpoint is reached or at the end of the treatment, the animals are sacrificed by cervical dislocation. The U251, U87, GSCs-U251 and GSCs-U87 cells are seeded at a density of 2×104 cells per well in 96-well plates separately, and incubated for 24 h. Cells are administered with Shikonin and Topotecan (0.02, 0.2, 2, 20, 40 μM). After the treatment, 10 μL of cell counting kit-8 (CCK-8) is added into each well for additional 1-hour incubation at 37°C. The optical density (OD) is read with a microplate reader at 450 nm[1]. Topoisomerase I \| \| \| \| \| \| \| \| \| \| [1]. Zhang FL, et al. PLoS One. 2013 Nov 26 8(11):e81815.Topoisomerase I inhibitors, Shikonin and Topotecan, inhibit growth and induce apoptosis of glioma cells andglioma stem cells. [Content Brief] [2]. Kumar S, et al. Metronomic oral topotecan with pazopanib is an active antiangiogenic regimen in mouse models of aggressive pediatric solid tumor. Clin Cancer Res. 2011 Sep 1 17(17):5656-67. [Content Brief]
Last Update	2025-04-01 14:45:47

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