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EC359

Catalog No. T11146 CAS 2012591-09-0

Synonyms: EC-359

EC359 is a potent and selective inhibitor of leukemia inhibitory factor receptor (LIFR), a potent inhibitor with anticancer activity, blocks LIF/LIFR interaction, and can be used in the study of leukemia and endometrial cancer.

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EC359, CAS 2012591-09-0

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1 mg	In stock	$ 399.00

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Purity: 98.11%

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Description	EC359 is a potent and selective inhibitor of leukemia inhibitory factor receptor (LIFR), a potent inhibitor with anticancer activity, blocks LIF/LIFR interaction, and can be used in the study of leukemia and endometrial cancer.
Targets&IC50	LIFR:10.2 nM (Kd)
In vitro	EC359 treatment (0-100 nM) for 3 days in BT-549, SUM-159, MDA-MB-231, MDA-MB-468, and HCC1806 cells leads to a dose-dependent reduction in cell viability[1]. In MDA-MB-231 and BT-549 cells, treatment with EC359 at concentrations of 20 nM and 25 nM for 72 hours significantly increases caspase-3/7 activity and the proportion of Annexin V-positive cells. EC359 exhibits noteworthy inhibitory activity on invasion and promotes apoptosis in triple-negative breast cancer (TNBC) cells[1].Treatment with EC359 at 100 nM for 12 hours in BT549 cells significantly decreases the expression of several known STAT3 target genes, including STAT1, TGFB1, JUNB, MCL-1, etc[1].In MDA-MB-231 and BT-549 cells, EC359 treatment at 100 nM for 1 hour substantially reduces STAT3 activation induced by LIF, OSM, and CNTF. Additionally, EC359 treatment leads to a significant decrease in the phosphorylation of AKT, mTOR, S6, and ERK1/2. Furthermore, EC359 treatment enhances the phosphorylation of proapoptotic p38MAPK in BT549 cells[1].
In vivo	Subcutaneous injection of EC359 at a dose of 5 mg/kg, administered three days per week for 25 days in female athymic nude mice, significantly reduces tumor progression. Importantly, the body weights of mice in the EC359-treated groups remain unchanged, confirming the low toxicity of EC359[1].

Synonyms	EC-359
Molecular Weight	540.68
Formula	C36H38F2O2
CAS No.	2012591-09-0

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (184.95 mM), Sonification is recommended.

References and Literature

1. Viswanadhapalli S, et al. EC359: A First-in-Class Small-Molecule Inhibitor for Targeting Oncogenic LIFR Signaling in Triple-Negative Breast Cancer. Mol Cancer Ther. 2019 Aug;18(8):1341-1354.

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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.

Keywords

EC359 2012591-09-0 Apoptosis Others EC-359 EC 359 inhibitor inhibit

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