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Exatecan Topoisomerase Inhibitor

Name: Exatecan
Brand: Selleck Chemicals
SKU: E5775
Rating: 5 (1 reviews)

Cat.No.: E5775

Exatecan (DX-8951) is a water-soluble derivative of camptothecin. It acts as an inhibitor of DNA topoisomerase I with an IC50 value of 1.906 μM. It demonstrates potent anti-tumour effects and triggers apoptotic cell death after treatment in human pancreatic cancer cells.

Chemical Structure

Molecular Weight: 435.45

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Quality Control

Batch: E577501 DMSO]21 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.78%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.78

Related Targets	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis PPAR Sirtuin Casein Kinase eIF
Other Topoisomerase Inhibitors	Camptothecin (CPT) Betulinic acid (S)-10-Hydroxycamptothecin Beta-Lapachone Ellagic acid Amonafide Voreloxin (SNS-595) hydrochloride Hydroxy Camptothecine Cu(II)-Elesclomol 7-Ethylcamptothecin

Chemical Information, Storage & Stability

Molecular Weight	435.45	Formula	C₂₄H₂₂FN₃O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	171335-80-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Solubility

In vitro
Batch:

DMSO : 21 mg/mL (48.22 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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.
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.	1.050mg/ml (2.41mM)	Taking the 1 mL working solution as an example, add 50 μL of 21 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.	0.250mg/ml (0.57mM)	Taking the 1 mL working solution as an example, add 50 μL of 5 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.

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	topoisomerase I 1.906 μM
References	[1] https://pubmed.ncbi.nlm.nih.gov/9330608/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-06-02)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT07454642	RECRUITING	Vulvar Adenocarcinoma; PDAC - Pancreatic Ductal Adenocarcinoma; Gastric Adenocarcinoma; GEJ Adenocarcinoma; Cervical Adenocarcinoma; Cervical Adenosquamous Carcinoma; Small Cell Carcinoma of Lung; Colorectal Cancer; Hormone Receptor Positive Breast Carcinoma	Avacta Life Sciences Ltd	2026-03-31	PHASE1
NCT07360314	RECRUITING	Advanced Solid Tumors	EMD Serono Research & Development Institute, Inc.	2026-02-13	PHASE1
NCT06730100	WITHDRAWN	Metastatic Mismatch Repair Proficient Colorectal Carcinoma; Refractory Mismatch Repair Proficient Colorectal Carcinoma; Stage IV Colorectal Cancer AJCC v8	National Cancer Institute (NCI)	2026-02-17	PHASE2
NCT05691517	RECRUITING	Advanced Malignant Solid Neoplasm; Metastatic Malignant Solid Neoplasm	National Cancer Institute (NCI)	2024-06-12	PHASE1
NCT00055939	COMPLETED	Sarcoma	Daiichi Sankyo	2003-01	PHASE2
NCT00055952	COMPLETED	Sarcoma	Daiichi Sankyo	2003-01	PHASE2

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