EAD1

Catalog No.S8576 Batch:S857601

Technical Data

Formula	C₂₆H₂₈Cl₂F₃N₇O₂
Molecular Weight	598.45	CAS No.	2320427-95-8
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (167.09 mM)
		Water	100 mg/mL (167.09 mM)
		Ethanol	100 mg/mL (167.09 mM)
* <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

EAD1 is a potent autophagy inhibitor with an IC50 of 5.8 μM in the BxPC3 cells. It has antiproliferative activities in lung and pancreatic cancer cells.

Targets

Autophagy ^[1]
(BxPC3 cells)

5.8 μM

In vitro

EAD1 inhibits autophagy, as judged by the cellular accumulation of the autophagy-related autophagosome proteins LC3-II and p62 and induces apoptosis^[1].

In vivo

EAD1 is a viable lead compound for evaluation of the antitumor activity of autophagy inhibitors in vivo^[1].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines H460 cells Concentrations 0-100 μM Incubation Time 24 h Method Cell growth inhibition is also assessed in a colony formation assay. H460 cells are plated at 250 cells per well in 24 well plates. After allowing for cell attachment overnight, HCQ and EAD1 are added at the indicated concentrations. After 24 hours, drug-containing medium is removed, and drug-free medium added. Cell colonies are stained with crystal violet after an additional 10-day growth in the absence of drug.

Cell Assay:^{^[1]}

Cell lines
H460 cells
Concentrations
0-100 μM
Incubation Time
24 h
Method
Cell growth inhibition is also assessed in a colony formation assay. H460 cells are plated at 250 cells per well in 24 well plates. After allowing for cell attachment overnight, HCQ and EAD1 are added at the indicated concentrations. After 24 hours, drug-containing medium is removed, and drug-free medium added. Cell colonies are stained with crystal violet after an additional 10-day growth in the absence of drug.

References

[1] Lars Ulrik Nordstrøm, et al. ACS Med Chem Lett. 2015, 6(2): 134-139.

Selleck's EAD1 has been cited by 2 publications

Radiosensitizing Pancreatic Cancer via Effective Autophagy Inhibition [ Mol Cancer Ther, 2022, 21(1):79-88]	PubMed: 34725193
GNS561, a clinical-stage PPT1 inhibitor, is efficient against hepatocellular carcinoma via modulation of lysosomal functions [ Autophagy, 2021, 1-17]	PubMed: 34740311

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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