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Artesunate ADC Cytotoxin inhibitor

Name: Artesunate
Brand: Selleck Chemicals
SKU: S2265
Availability: InStock
Rating: 5 (17 reviews)

Cat.No.S2265

Artesunate is a part of the artemisinin group of agents with an IC50 of < 5 μM for small cell lung carcinoma cell line H69. It is a potential inhibitor of STAT-3 and exhibits selective cytotoxicity of cancer cells over normal cells in vitro; this compound is a potent inhibitor of EXP1.

Chemical Structure

Molecular Weight: 384.42

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Quality Control

Batch: Purity: 99.56%

99.56

Related Targets	EGFR JAK STAT Pim
Other ADC Cytotoxin Inhibitors	Triptolide SN-38 Luteolin (+)-Bicuculline Rutin Artemisinin Pinocembrin Harmine hydrochloride Luteoloside BHQ

Solubility

In vitro
Batch:

DMSO : 77 mg/mL (200.3 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 77 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection 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.	3.850mg/ml (10.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 77 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.	3.850mg/ml (10.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 77 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.
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.

Chemical Information, Storage & Stability

Molecular Weight	384.42	Formula	C₁₉H₂₈O₈	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	88495-63-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

Targets/IC₅₀/Ki	EXP1(a membrane glutathione S-transferase) STAT3
In vitro	ART could alter the biomechanical properties of the glioma cells to inhibit cell proliferation, migration and invasion . This compound significantly suppresses the cell proliferation, induces the apoptosis and promoted cell cycle arrest at G0/G1 phase in SKM-1 cells. The mechanisms of its anti-MDS is associated with the increase of intracellular calciumion concentration and ROS levels. In addition, the pro-apoptotic activity of this chemical may be involved in the regulation of BCL-2 /BAX ratio and the expressions of P-bad and survivin. Its treatment demethylates CDH1, which, in turn recovers the E-cadherin activation in SKM-1 cells.
In vivo	Artesunate is a medication used to treat malaria. This compound can induce radiosensitivity of HeLa cells in vivo using Xenograft model of nude mice. It had a relatively high immunosuppressive activity with low toxicity, and could inhibit T lymphocyte proliferation induced by mitogen and alloantigen.
References	[1] https://pubmed.ncbi.nlm.nih.gov/26078714/ [2] https://pubmed.ncbi.nlm.nih.gov/27279152/ [3] https://pubmed.ncbi.nlm.nih.gov/26913409/ [4] https://pubmed.ncbi.nlm.nih.gov/25126794/ [5] https://pubmed.ncbi.nlm.nih.gov/24666614/ [6] https://pubmed.ncbi.nlm.nih.gov/23583335/ [7] https://pubmed.ncbi.nlm.nih.gov/26873192/

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05929157	Not yet recruiting	Severe Malarial Treatment	Centre de Recherche Médicale de Lambaréné\|Institute of Tropical Medicine University of Tuebingen	September 1 2023	Phase 1\|Phase 2
NCT05555862	Active not recruiting	Anal High Grade Squamous Intraepithelial Lesion\|Anal Precancerous Condition\|AIN 2/3\|HPV Infection\|Anal Dysplasia\|HPV Disease	Frantz Viral Therapeutics LLC\|Amarex CRO\|University of California San Francisco\|Anal Dysplasia Clinic MidWest\|Laser Surgery Care	February 10 2023	Phase 2
NCT04921930	Recruiting	Friedreich Ataxia	Institut National de la Santé Et de la Recherche Médicale France\|Imagine Institute	May 6 2022	Phase 1\|Phase 2
NCT05343312	Active not recruiting	Malaria	Centro de Investigacao em Saude de Manhica\|United States Agency for International Development (USAID)	March 16 2022	Phase 4

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