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Topotecan Topoisomerase inhibitor

Name: Topotecan
Brand: Selleck Chemicals
SKU: S9321
Availability: InStock
Rating: 5 (32 reviews)

Cat.No.S9321

Topotecan(NSC609699,Nogitecan,SKFS 104864A) is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases.

Chemical Structure

Molecular Weight: 421.45

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.94%

99.94

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Chemical Information, Storage & Stability

Molecular Weight	421.45	Formula	C₂₃H₂₃N₃O₅	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	123948-87-8	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NSC609699,Nogitecan,SKFS 104864A			Smiles	CCC1(C2=C(COC1=O)C(=O)N3CC4=CC5=C(C=CC(=C5CN(C)C)O)N=C4C3=C2)O

Solubility

In vitro
Batch:

DMSO : 84 mg/mL (199.31 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : ˂1 mg/mL

Ethanol : ˂1 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.100mg/ml (4.98mM)	Taking the 1 mL working solution as an example, add 50 μL of 42 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.150mg/ml (0.36mM)	Taking the 1 mL working solution as an example, add 50 μL of 3 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Topo I ^[1]
In vitro	Topotecan exhibits inhibition of outgrowth of the highly invasive and migratory leader cells (LC) population, however, topotecan enrichs the LC subset 20% above the untreated control level.^[2]
In vivo	Topotecan (TPT), at least in part by inhibiting expression of Fli-1, significantly ameliorates lupus nephritis in NZBWF1 mice as effectively or better than cyclophosphamide (CYC).^[3]
References	[1] https://pubmed.ncbi.nlm.nih.gov/29412654/ [2] https://pubmed.ncbi.nlm.nih.gov/34470672/ [3] https://pubmed.ncbi.nlm.nih.gov/33559345/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04455139	Terminated	Eye Cancer Retinoblastoma	Prof. Beck Popovic Maja\|University of Lausanne Hospitals	November 15 2021	Phase 2
NCT05083000	Unknown status	COVID-19 Respiratory Infection	National University Hospital Singapore\|Christian Medical College Vellore India	August 16 2021	Phase 1
NCT04156347	Active not recruiting	Retinoblastoma	Targeted Therapy Technologies LLC	June 16 2021	Phase 1
NCT04428879	Recruiting	Retinoblastoma	The Hospital for Sick Children	June 16 2020	Phase 1

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