Topotecan HCl

貨號 Cat. No.: S1231
規格 Size: 5~200mg
品牌 Brand: Selleckchem

Description

Topotecan HCl

Catalog No.S12312 Product Citations

Topotecan (NSC 609699) is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM, respectively.

Size

Price

Stock

Quantity

10mM/1mLIn DMSO	USD 289	In stock	0 1 2 3 4 5 6 7 8 9 10
50mg	USD 226	In stock	0 1 2 3 4 5 6 7 8 9 10
100mg	USD 403	In stock	0 1 2 3 4 5 6 7 8 9 10

Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

Biological Activity

Description	Topotecan (NSC 609699) is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM, respectively.
Targets	MCF-7 Luc cells	DU-145 Luc cells
IC50	13 nM	2 nM ^[1]
In vitro	Stronger drug activity of Topotecan is observed for DU-145 Luc and MCF-7 Luc cells. ^[1] Topotecan causes cytotoxicity during the course of DNA replication by stabilizing the covalent complex between topoisomerase I and DNA and preventing the religation of enzyme-linked single-strand DNA break. Topotecan stabilizes topoisomerase I/DNA cleavable complexes in radiation-resistant human B-lineage acute lymphoblastic leukemia (ALL) cells, causes rapid apoptotic cell death despite high-level expression of bcl-2 protein, and inhibits ALL cell clonogenic growth in a dose-dependent fashion. ^[2]
In vivo	Animals inoculate s.c. with DU-145 Luc cells and then treated with Topotecan demonstrates significant tumor growth and regression as measured with calipers and luminescent imaging. The correlation coefficient is 0.75 for the control untreated group and 0.93 for the Topotecan-treated group. Similarly, tumor progression and regression are measurable using luminescent imaging for untreated and Topotecan-treated mice inoculated i.p. with MCF-7 Luc cells. ^[1] Topotecan elicited potent antileukemic activity in severe combined immune-deficiency (SCID) mouse models of human poor prognosis ALL. Topotecan markedly improved event-free survival of SCID mice challenged with otherwise fatal doses of humaln leukemia cells at systemic drug exposure levels. ^[2] Gliomas preferentially express TRAIL R2 and that treatment with Topotecan significantly up-regulates its expression. ^[3]
Features	Topotecan is a water-soluble derivative of camptothecin.

Protocol(Only for Reference)

Cell Assay: ^[1]

Cell lines	MCF-7 Luc and DU-145 Luc cells
Concentrations	0 μg/mL - 0.692 μg/mL
Incubation Time	96 hours
Method	Topotecan is dissolved in sterile water to a stock concentration of 1 mg/mL, diluted to 6 μg/mL in cultured medium and then serially diluted 1:4 in opaque, white tissue culture-treated microplates to a final volume of 0.1 mL/well. MCF-7 Luc and DU-145 Luc cells are resuspended in 3×10⁴ cells/mL in DMEM with high glucose containing 10% FBS and 0.5 mg/mL Geneticin; 100 μL of cells are added in each well. Plates are incubated for 4 days at 37 °C in 95% humidity/5% CO₂. After incubation, 0.05 mL of 0.1 M HEPES buffer (pH 7.9) containing 50 μg/mL D-luciferin is added to each well. After incubation at room temperature for 10 minutes, the culture microplate is measured in a microplate luminometer and a molecular light imager. Results obtained with the microplate luminometer are calculated using no inhibition control wells without exogenous drug and maximum inhibition control wells containing ATP inhibitor. Results for the molecular light imager are similarly calculated using values obtained with a 5 minutes luminescent i

Animal Study: ^[1]

Animal Models	Mice with MCF-7 Luc or DU-145 Luc cells
Dosages	0.25 mg/mL
Administration	Administered via i.p.
Solubility	Saline, 30 mg/mL

References

Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number	Recruitment	Conditions	Sponsor /Collaborators	Start Date	Phases
NCT01840943	Recruiting	Epithelial Ovarian Cancer	Xian-Janssen Pharmaceutical Ltd.	2013-06	Phase 3
NCT01904253	Recruiting	Small Cell Lung Cancer (SCLC)	Taiho Pharma USA, Inc.\|Taiho Pharmaceutical Co., Ltd.	2013-07	Phase 2
NCT01795430	Recruiting	Adult Supratentorial Primitive Neuroectodermal Tumor (PNET)\|Ewing Sarcoma of Bone\|Extraosseous Ewing Sarcoma\|Metastatic Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor\|Recurrent Childhood Sup	City of Hope Medical Center\|National Cancer Institute (NCI)	2013-07
NCT01931098	Recruiting	Brain Neoplasms\|Central Nervous System Neoplasms	M.D. Anderson Cancer Center\|BRAIN TUMOR TRIALS COLLABORATIVE (BTTC)\|GlaxoSmithKline	2013-11	Phase 2
NCT01987596	Recruiting	Childhood Central Nervous System Choriocarcinoma\|Childhood Central Nervous System Germinoma\|Childhood Central Nervous System Mixed Germ Cell Tumor\|Childhood Central Nervous System Teratoma\|Childhood C	Barbara Ann Karmanos Cancer Institute\|National Cancer Institute (NCI)\|Children’s Hospital of Michigan	2013-11	Phase 3

Chemical Information

Download Topotecan HCl SDF

Molecular Weight (MW)	457.91
Formula	C₂₃H₂₃N₃O₅.HCl
CAS No.	119413-54-6

Storage	3 years -20â„ƒPowder
Storage	6 months-80â„ƒin DMSO
Syonnyms	Hycamtin, NSC 609699

Solubility (25°C) *	In vitro	DMSO	92 mg/mL (200 mM)
		Water	92 mg/mL (200 mM)
		Ethanol	<1 mg/mL (<1 mM)
	In vivo	Saline,	30 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.