Alantolactone

Catalog No.S8318 Batch:S831801

Technical Data

Formula	C₁₅H₂₀O₂
Molecular Weight	232.32	CAS No.	546-43-0
Solubility (25°C)*	In vitro	DMSO	46 mg/mL (198.0 mM)
		Ethanol	46 mg/mL (198.0 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

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

Targets

STAT3 ^[1]

activin/SMAD3 ^[3]

In vitro

Alantolactone selectively suppresses STAT3 activation and exhibits potent anticancer activity in MDA-MB-231 cells. Alantolactone 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. Alantolactone 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. Alantolactone treatment resulted in the inhibition of migration, invasion, adhesion, and colony formation^[1]. Alantolactone could induce activin signaling and activin target gene expression. Alantolactone 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]. Alantolactone 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. Alantolactone can cross blood-brain barrier^[2].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines MDA-MB-231 and MCF-7 cells Concentrations 15 μM Incubation Time 24 h Method Cell viability was evaluated using MTT assay. The cells were seeded into 96-well plates and maintained at 37 °C for 24 h. The cells were treated with alantolactone for 24 h. The MTT solution (0.5 mg/mL) was added to each well, and the cells were incubated for another 3 h. The MTT formazan crystals were dissolved in DMSO. The results were obtained by measuring the absorbance at a wavelength of 540 nm using a microplate reader.
Animal Study:^{^[1]}	Animal Models athymic BALB/c nude mice Dosages 2.5 mg/kg Administration i.p.

Cell Assay:^{^[1]}

Cell lines
MDA-MB-231 and MCF-7 cells
Concentrations
15 μM
Incubation Time
24 h
Method
Cell viability was evaluated using MTT assay. The cells were seeded into 96-well plates and maintained at 37 °C for 24 h. The cells were treated with alantolactone for 24 h. The MTT solution (0.5 mg/mL) was added to each well, and the cells were incubated for another 3 h. The MTT formazan crystals were dissolved in DMSO. The results were obtained by measuring the absorbance at a wavelength of 540 nm using a microplate reader.

Animal Study:^{^[1]}

Animal Models
athymic BALB/c nude mice
Dosages
2.5 mg/kg
Administration
i.p.

References

Customer Product Validation

: Data from [Data independently produced by , , Onco Targets Ther, 2017, 10:1767-1776]

Selleck's Alantolactone has been cited by 2 publications

Grainyhead 1 acts as a drug-inducible conserved transcriptional regulator linked to insulin signaling and lifespan [ Nat Commun, 2022, 13(1):107]	PubMed: 35013237
Niclosamide inhibition of STAT3 synergizes with erlotinib in human colon cancer [Shi L Onco Targets Ther, 2017, 10:1767-1776]	PubMed: 28367059

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SHIPPING AND STORAGE
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