Topotecan hydrochloride (Synonyms: SKF 104864A hydrochloride; NSC 609669 hydrochloride)

Name: Topotecan hydrochloride
Brand: MedChemExpress
SKU: HY-13768A
Rating: 5.0 (28 reviews)

Cat. No.: HY-13768A Purity: 99.89%: FAQs
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Topotecan Hydrochloride (SKF 104864A Hydrochloride) is a Topoisomerase I inhibitor with potent antineoplastic activities.

For research use only. We do not sell to patients.

Topotecan hydrochloride Chemical Structure

CAS No. : 119413-54-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 38	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 137	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
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Based on 28 publication(s) in Google Scholar

Other Forms of Topotecan hydrochloride:

Topotecan Get quote
Topotecan hydrochloride hydrate Get quote
Topotecan hydrochloride (Standard) Get quote

26 Publications Citing Use of MCE Topotecan hydrochloride

: Topotecan hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Aug 21;10(1):3761. [Abstract]; WDR5 inhibitor OICR-9429 enhances the sensitivity of ovarian cancer to genotoxic chemotherapeutics in vivo. Representative images and the apoptotic rate the indicated chemotherapy-treated xenograft tumors.

: Topotecan hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Aug 21;10(1):3761. [Abstract]; IB analysis of the level of cleaved-caspase 3 and cleaved-PARP1 in the indicated chemotherapy-treated xenograft tumors. GAPDH served as the loading control.

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Topoisomerase Topo I Topo II

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Topotecan Hydrochloride (SKF 104864A Hydrochloride) is a Topoisomerase I inhibitor with potent antineoplastic activities.

IC₅₀ & Target^[1]

Topoisomerase I

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	0.162 μM Compound: Topotecan	Cytotoxicity against human A375 cells after 24 hrs by MTT assay Cytotoxicity against human A375 cells after 24 hrs by MTT assay	[PMID: 24980118]
Bel-7402	IC₅₀	0.4 μg/mL Compound: Topotecan	In vitro cytotoxicity against Bel7402 cell line (human liver cancer) using MTT assay In vitro cytotoxicity against Bel7402 cell line (human liver cancer) using MTT assay	[PMID: 15225719]
Caco-2	IC₅₀	0.119 μM Compound: Topotecan	Cytotoxicity against human Caco2 cells after 24 hrs by MTT assay Cytotoxicity against human Caco2 cells after 24 hrs by MTT assay	[PMID: 24980118]
HCT-8	IC₅₀	0.03 μg/mL Compound: Topotecan	In vitro cytotoxicity against HCT-8 cell line (human colon cancer) using MTT assay In vitro cytotoxicity against HCT-8 cell line (human colon cancer) using MTT assay	[PMID: 15225719]
HCT-8	IC₅₀	1.875 μM Compound: 3, Topotecan	Antiproliferative activity against human HCT8 cells after 48 hrs by CCK8 assay Antiproliferative activity against human HCT8 cells after 48 hrs by CCK8 assay	[PMID: 25481395]
HeLa	IC₅₀	0.38 μM Compound: Topotecan	Cytotoxicity against human HeLa cells after 24 hrs by MTT assay Cytotoxicity against human HeLa cells after 24 hrs by MTT assay	[PMID: 24980118]
HepG2	IC₅₀	4.208 μM Compound: 3, Topotecan	Antiproliferative activity against human HepG2 cells after 48 hrs by CCK8 assay Antiproliferative activity against human HepG2 cells after 48 hrs by CCK8 assay	[PMID: 25481395]
Jurkat	IC₅₀	0.127 μM Compound: Topotecan	Cytotoxicity against human Jurkat cells after 24 hrs by MTT assay Cytotoxicity against human Jurkat cells after 24 hrs by MTT assay	[PMID: 24980118]
KB	IC₅₀	0.02 μg/mL Compound: Topotecan	In vitro cytotoxicity against KB cell line (human epidermoid carcinoma of the nasopharynx) using MTT assay In vitro cytotoxicity against KB cell line (human epidermoid carcinoma of the nasopharynx) using MTT assay	[PMID: 15225719]
KB	IC₅₀	2.282 μM Compound: 3, Topotecan	Antiproliferative activity against human KB cells after 48 hrs by CCK8 assay Antiproliferative activity against human KB cells after 48 hrs by CCK8 assay	[PMID: 25481395]
MDA-MB-231	IC₅₀	0.473 μM Compound: Topotecan	Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay	[PMID: 24980118]
NCI-H460	IC₅₀	0.61 μM Compound: 2	Antiproliferative activity against human NCI-H460 cells after short term exposure for 1 hr measured after 72 hrs in drug-free medium Antiproliferative activity against human NCI-H460 cells after short term exposure for 1 hr measured after 72 hrs in drug-free medium	[PMID: 19530720]
SGC-7901	IC₅₀	2.292 μM Compound: 3, Topotecan	Antiproliferative activity against human SGC7901 cells after 48 hrs by CCK8 assay Antiproliferative activity against human SGC7901 cells after 48 hrs by CCK8 assay	[PMID: 25481395]

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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

457.91

Formula

C₂₃H₂₄ClN₃O₅

CAS No.

119413-54-6

Appearance

Solid

Color

Off-white to yellow

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

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (218.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 33.33 mg/mL (72.79 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1838 mL	10.9192 mL	21.8384 mL
5 mM	0.4368 mL	2.1838 mL	4.3677 mL
10 mM	0.2184 mL	1.0919 mL	2.1838 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.46 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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(per animal)

μL

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.89%

Select Batch:

Data Sheet (284 KB) SDS (480 KB)

COA (256 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[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]

Cell Assay ^[1]	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 Hydrochloride (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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[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 Hydrochloride + 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 or Pulse TP (15 mg/kg Topotecan). 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.1838 mL	10.9192 mL	21.8384 mL	54.5959 mL
	5 mM	0.4368 mL	2.1838 mL	4.3677 mL	10.9192 mL
	10 mM	0.2184 mL	1.0919 mL	2.1838 mL	5.4596 mL
	15 mM	0.1456 mL	0.7279 mL	1.4559 mL	3.6397 mL
	20 mM	0.1092 mL	0.5460 mL	1.0919 mL	2.7298 mL
	25 mM	0.0874 mL	0.4368 mL	0.8735 mL	2.1838 mL
	30 mM	0.0728 mL	0.3640 mL	0.7279 mL	1.8199 mL
	40 mM	0.0546 mL	0.2730 mL	0.5460 mL	1.3649 mL
	50 mM	0.0437 mL	0.2184 mL	0.4368 mL	1.0919 mL
	60 mM	0.0364 mL	0.1820 mL	0.3640 mL	0.9099 mL
DMSO	80 mM	0.0273 mL	0.1365 mL	0.2730 mL	0.6824 mL
DMSO	100 mM	0.0218 mL	0.1092 mL	0.2184 mL	0.5460 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Topotecan hydrochloride Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Topotecan119413-54-6SKF 104864ANSC 609669NSC609669NSC-609669TopoisomeraseAutophagyApoptosisInhibitorinhibitorinhibit

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Topotecan hydrochloride (Synonyms: SKF 104864A hydrochloride; NSC 609669 hydrochloride)

Customer Review

Other Forms of Topotecan hydrochloride:

Topotecan hydrochloride Related Antibodies

26 Publications Citing Use of MCE Topotecan hydrochloride

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Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Topotecan hydrochloride Related Antibodies

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Complete Stock Solution Preparation Table

Topotecan hydrochloride Related Classifications

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