Topotecan HCl

Catalog No.S1231

Topotecan HCl is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively.

Price Stock Quantity  
USD 230 In stock
USD 180 In stock
USD 320 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

Topotecan HCl Chemical Structure

Topotecan HCl Chemical Structure
Molecular Weight: 457.91

Validation & Quality Control

2 customer reviews :

Quality Control & MSDS

Related Compound Libraries

Product Information

  • Compare Topoisomerase Inhibitors
    Compare Topoisomerase Products
  • Research Area
  • Topotecan HCl Mechanism

Product Description

Biological Activity

Description Topotecan HCl is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively.
Targets Topo I (DU-145 Luc cells) [1]
(Cell-free assay)
Topo I (MCF-7 Luc cells) [1]
(Cell-free assay)
IC50 2 nM 13 nM
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:


Cell lines MCF-7 Luc and DU-145 Luc cells
Concentrations 0 μg/mL - 0.692 μg/mL
Incubation Time 96 hours

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 imager.

Animal Study:


Animal Models Mice with MCF-7 Luc or DU-145 Luc cells
Formulation PBS
Dosages 0.25 mg/mL
Administration Administered via i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Caceres G, et al. Anticancer Drugs. 2003, 14(7), 569-574.

[2] Uckun FM, et al. Blood. 1995. 85(10), 2817-2828.

view more

Clinical Trial Information( data from, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT02348398 Not yet recruiting Cervical Cancer M.D. Anderson Cancer Center|GlaxoSmithKline August 2016 Phase 2
NCT02822157 Not yet recruiting Ovarian Epithelial Cancer Universitaire Ziekenhuizen Leuven|AstraZeneca August 2016 Phase 2
NCT02566993 Not yet recruiting Small-cell Lung Cancer PharmaMar July 2016 Phase 3
NCT02813135 Recruiting Children, Adolescents and Young Adults With Refractory or Recurrent Malignancies Gustave Roussy, Cancer Campus, Grand Paris|National Cance  ...more Gustave Roussy, Cancer Campus, Grand Paris|National Cancer Institute, France June 2016 Phase 1|Phase 2
NCT02786719 Recruiting Neuroblastoma Baylor College of Medicine|Texas Childrens Hospital June 2016 --

view more

Chemical Information

Download Topotecan HCl SDF
Molecular Weight (MW) 457.91


CAS No. 119413-54-6
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms NSC609699, Nogitecan HCl, SKFS 104864A
Solubility (25°C) * In vitro DMSO 92 mg/mL (200.91 mM)
Water 92 mg/mL (200.91 mM)
Ethanol <1 mg/mL
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.
Chemical Name (4S)​-10-​[(dimethylamino)​methyl]​-​4-​ethyl-​4,​9-​dihydroxy-​1H-​pyrano[3',​4':6,​7]​indolizino[1,​2-​b]​quinoline-​3,​14(4H,​12H)​-​dione, hydrochloride (1:1)

Frequently Asked Questions

  • Question 1
    I would like get the compound for mice intraperitoneally injection, What would you recommend to improve solubility? What could I use as solvent (%v?) that is nontoxic (unlike Methanol) and could be injected into mice intraperitoneally?

    Answer: Topotecan HCl is generally prepared by Saline for I.P. administration.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related Topoisomerase Products

  • SCR7

    SCR7 is a specific DNA Ligase IV inhibitor, which blocks nonhomologous end-joining (NHEJ).

  • Blasticidin S HCl

    Blasticidin S HCl is a nucleoside antibiotic isolated from Stretomyces girseochromogenes, and acts as a DNA and protein synthesis inhibitor, used to select transfected cells carrying bsr or BSD resistance genes.

  • LMK-235

    LMK-235 is a selective inhibitor of HDAC4 and HDAC5 with IC50 of 11.9 nM and 4.2 nM, respectively.

  • Doxorubicin (Adriamycin)

    Doxorubicin (Adriamycin) is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis in tumor cells.

  • Etoposide

    Etoposide is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity.

  • Irinotecan

    Irinotecan is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively.

    Features:Irinotecan is a prodrug that is used to treat metastatic colorectal cancer.

  • Camptothecin

    Camptothecin is a specific inhibitor of DNA topoisomerase I (Topo I) with IC50 of 0.68 μM in a cell-free assay. Phase 2.

  • Daunorubicin HCl

    Daunorubicin HCl inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM in a cell-free assay.

  • SN-38

    SN-38 is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks.

  • Idarubicin HCl

    Idarubicin HCl is a hydrochloride salt form of Idarubicin which is an anthracycline antibiotic and a DNA topoisomerase II (topo II) inhibitor for MCF-7 cells with IC50 of 3.3 ng/mL in a cell-free assay.

    Features:Idarubicin is a substrate for CYP450 2D6 and 2C9.

Recently Viewed Items

Tags: buy Topotecan HCl | Topotecan HCl ic50 | Topotecan HCl price | Topotecan HCl cost | Topotecan HCl solubility dmso | Topotecan HCl purchase | Topotecan HCl manufacturer | Topotecan HCl research buy | Topotecan HCl order | Topotecan HCl mouse | Topotecan HCl chemical structure | Topotecan HCl mw | Topotecan HCl molecular weight | Topotecan HCl datasheet | Topotecan HCl supplier | Topotecan HCl in vitro | Topotecan HCl cell line | Topotecan HCl concentration | Topotecan HCl nmr
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us