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Exatecan

Name: Exatecan
Brand: TargetMol
SKU: T11249
Price: 29 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T11249Cas No. 171335-80-1

Alias DX-8951f

Exatecan (DX-8951f) is a DNA topoisomerase I (TOP1) inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL).Exatecan has antitumor activity and may be used in cancer research.

Exatecan

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Purity: 99.96%

Catalog No. T11249Alias DX-8951fCas No. 171335-80-1

Exatecan (DX-8951f) is a DNA topoisomerase I (TOP1) inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL).Exatecan has antitumor activity and may be used in cancer research.

Pack Size	Price	USA Warehouse	Global Warehouse
10 mg	$30	In Stock	In Stock
25 mg	$64	In Stock	In Stock
50 mg	$93	In Stock	In Stock
100 mg	$138	In Stock	In Stock
500 mg	$339	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$29	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.96%

Appearance:Solid

Resource Download

COA HPLC HNMR

Product Introduction

Bioactivity

Description	Exatecan (DX-8951f) is a DNA topoisomerase I (TOP1) inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL).Exatecan has antitumor activity and may be used in cancer research.
Targets&IC50	Topo I:2.2 μM
In vitro	Exatecan (DX-8951f) displays cytotoxic activities against PC-6, and PC-6/SN2-5 cells, with mean GI50s of 0.186 and 0.395 ng/mL, respectively.[2] Exatecan (34 nM) stabilizes DNA-TopoI complexes in PC-6 and PC-6/SN2-5 cells.[2] Exatecan is a potent topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL.[2] Exatecan significantly inhibits the proliferation of several cancer cell lines, with mean GI50s of 2.02 ng/mL, 2.92 ng/mL, 1.53 ng/mL, and 0.877 ng/mL for breast cancer cells, colon cancer cells, stomach cancer cells, and lung cancer cells, respectively.[2]
In vivo	Exatecan (DX-8951f) (3.325-50 mg/kg; i.v.) exhibits antitumor activities in the mice model bearing tumor cells, without toxic death.[3] Exatecan (15, 25 mg/kg; i.v.) highly inhibits MIA-PaCa, BxPC-3 primary tumor growth in the MIA-PaCa-2 early-stage model and early-stage model of BxPC-3. Exatecan also significantly suppresses BxPC-3 lymphatic metastasis and completely eliminates lung metastasis in the BxPC-3 late-stage cancer model.[3]
Synonyms	DX-8951f

Chemical Properties

Molecular Weight	435.45
Formula	C₂₄H₂₂FN₃O₄
Cas No.	171335-80-1
Smiles	N[C@@H]1C2=C3C(C=4N(C3)C(=O)C5=C(C4)[C@](CC)(O)C(=O)OC5)=NC=6C2=C(CC1)C(C)=C(F)C6
Relative Density.	1.53 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 20 mg/mL (45.93 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2965 mL	11.4824 mL	22.9647 mL	114.8237 mL
5 mM	0.4593 mL	2.2965 mL	4.5929 mL	22.9647 mL
10 mM	0.2296 mL	1.1482 mL	2.2965 mL	11.4824 mL
20 mM	0.1148 mL	0.5741 mL	1.1482 mL	5.7412 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc