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Alantolactone TGF-beta/Smad modulator

Name: Alantolactone
SKU: S8318
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S8318

Alantolactone, a naturally occurring eudesmane-type sesquiterpene lactone (SL), could induce activin/SMAD3 signaling and disrupt Cripto-1/activin receptor type II A interaction.

Chemical Structure

Molecular Weight: 232.32

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

Quality Control

Batch: Purity: 99.98%

99.98

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Chemical Information, Storage & Stability

Molecular Weight	232.32	Formula	C₁₅H₂₀O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	546-43-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Solubility

In vitro
Batch:

DMSO : 46 mg/mL (198.0 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 46 mg/mL

Water : 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 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.300mg/ml (9.90mM)	Taking the 1 mL working solution as an example, add 50 μL of 46 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.
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.	2.300mg/ml (9.90mM)	Taking the 1 mL working solution as an example, add 50 μL of 46 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.
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	STAT3 ^[1] activin/SMAD3 ^[3]
In vitro	Alantolactone selectively suppresses STAT3 activation and exhibits potent anticancer activity in MDA-MB-231 cells. This compound effectively suppressed both constitutive and inducible STAT3 activation at tyrosine 705. It decreased STAT3 translocation to the nucleus, its DNA-binding, and STAT3 target gene expression. This chemical significantly inhibits STAT3 activation with a marginal effect on MAPKs and on NF-κB transcription; however, this effect is not mediated by inhibiting STAT3 upstream kinases. SHP-1, SHP-2, and PTEN, which are protein tyrosine phosphatases (PTPs) were not affected by alantolactone. Its treatment resulted in the inhibition of migration, invasion, adhesion, and colony formation^[1]. It could induce activin signaling and activin target gene expression. This agent activated the activin signaling pathway in a cancer cell line. It could promote SMAD2/3 nuclear translocation in a very short time^[3].
In vivo	In vivo administration of alantolactone inhibited the growth of human breast xenograft tumors^[1]. This compound exerts no toxic effect on liver and kidneys in vivo, The drug was well tolerated by mice and no mortality or any sign of pharmacotoxicity was found at a dose of 100 mg/kg during all the experimental periods. It can cross blood-brain barrier^[2].
References	[1] https://pubmed.ncbi.nlm.nih.gov/25434800/ [2] https://pubmed.ncbi.nlm.nih.gov/22837216/ [3] https://pubmed.ncbi.nlm.nih.gov/21378277/

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