Home DNA Damage/DNA Repair Topoisomerase inhibitor Exatecan Mesylate For research use only.

Exatecan Mesylate

Synonyms: DX-8951 Mesylate

Exatecan Mesylate (DX-8951f) is a water-soluble and non-pro-drug analog of camptothecin and shows significant topoisomerase I inhibition with IC50 of 0.975 μg/ml.

Exatecan Mesylate Chemical Structure

Exatecan Mesylate Chemical Structure

CAS No. 169869-90-3

Purity & Quality Control

Batch: S899901 DMSO]12.5 mg/mL]false]Water]12.5 mg/mL]false]Ethanol]Insoluble]false Purity: 99.97%
99.97

Exatecan Mesylate Related Products

Signaling Pathway

Topoisomerase Signaling Pathways

Topoisomerase Signaling Pathway

Biological Activity

Description Exatecan Mesylate (DX-8951f) is a water-soluble and non-pro-drug analog of camptothecin and shows significant topoisomerase I inhibition with IC50 of 0.975 μg/ml.
Targets
topoisomerase I [1]
In vitro
In vitro

Exatecan Mesylate shows both high potency against a series of 32 malignant cell lines and significant topoisomerase I inhibition in vitro. The anti‐proliferative activity of Exatecan Mesylate is about 6 and 28 times greater than that of SN‐38 or SK&F 10486‐A, respectively.[1]
In Vivo
In vivo

In mice, the antitumor activity of three doses of Exatecan Mesylate administered i.v. at 4‐day intervals against human gastric adenocarcinoma SC‐6 xenografts is greater than that of CPT‐11 or SK&F 10486‐A. Moreover, it overcame P‐glycoprotein‐mediated multi‐drug resistance. These data suggest that Exatecan Mesylate has a high antitumor activity and is a potential therapeutic agent.[1]
Animal Research Animal Models Mouse
Dosages 3.325 mg/kg to 50 mg/kg
Administration i.v.

Chemical Information & Solubility

Molecular Weight 531.55 Formula

C24H22FN3O4.CH4O3S
CAS No. 169869-90-3 SDF --
Smiles CCC1(O)C(=O)OCC2=C1C=C3N(CC4=C5C(N)CCC6=C5C(=CC(=C6C)F)N=C34)C2=O.C[S](O)(=O)=O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 12.5 mg/mL ( (23.51 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 12.5 mg/mL

Ethanol : Insoluble


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In vivo
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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.
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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.

Handling Instructions

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