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  3. EC359

EC359 

Cat. No.: HY-120142
Handling Instructions

EC359 is a potent, selective, high affinity and orally active leukemia inhibitory factor receptor (LIFR) inhibitor with a Kd of 10.2 nM, which directly interacts with LIFR to effectively block LIF/LIFR interactions.

For research use only. We do not sell to patients.

EC359 Chemical Structure

EC359 Chemical Structure

CAS No. : 2012591-09-0

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Description

EC359 is a potent, selective, high affinity and orally active leukemia inhibitory factor receptor (LIFR) inhibitor with a Kd of 10.2 nM, which directly interacts with LIFR to effectively block LIF/LIFR interactions[1].

IC50 & Target

Kd: 10.2 nM (leukemia inhibitory factor receptor)[1]

In Vitro

EC359 (0-100 nM; 3 days; BT-549, SUM-159, MDA-MB-231, MDA-MB-468, and HCC1806 cells) treatment reduces cell viability in a dose-dependent manner[1].
EC359 (20 nM, 25 nM; 72 hours; MDA-MB-231 and BT-549 cells) treatment significantly increases caspase-3/7 activity and Annexin V-positive cells in both MDAMB-231 and BT-549 cells. EC359 exhibits significant inhibitory activity on invasion and promotes apoptosis of TNBC cells[1].
EC359 (100 nM; 12 hours; BT549 cells) treatment significantly reduces the expression of several (such as STAT1 TGFB1, JUNB, MCL-1, etc) known STAT3 target genes[1].
EC359(100 nM; 1 hour; MDA-MB-231 and BT-549 cells) treatment substantially reduces the LIF activation of STAT3, also reduces the STAT3 activation by OSM and CNTF. EC359 treatment substantially decreases the phosphorylation of AKT, mTOR, S6, and ERK1/2 in MDA-MB231 and BT-549 cells. EC359 treatment also increases the phosphorylation of proapoptotic p38MAPK in BT549 cells[1].

Cell Viability Assay[1]

Cell Line: BT-549, SUM-159, MDA-MB-231, MDA-MB-468, and HCC1806 cells
Concentration: 0 nM, 1.5 nM, 12.5 nM, 25 nM, 50 nM, 100 nM
Incubation Time: 3 days
Result: Reduced cell viability in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 and BT-549 cells
Concentration: 20 nM, 25 nM
Incubation Time: 72 hours
Result: Promoted apoptosis of TNBC cells.

RT-PCR[1]

Cell Line: BT549 cells
Concentration: 100 nM
Incubation Time: 12 hours
Result: Reduced the expression of several known STAT3 target genes.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 and BT-549 cells
Concentration: 100 nM
Incubation Time: 1 hour
Result: Substantially reduced the LIF activation of STAT3, reduced the STAT3 activation by OSM and CNTF, decreased the phosphorylation of AKT, mTOR, S6, and ERK1/2 in both BT-549 and MDA-MB-231 cells and increased the phosphorylation of proapoptotic p38MAPK in BT549 cells.
In Vivo

EC359 (5 mg/kg; subcutaneous injection; 3 days per week; for 25 days; female athymic nude mice) treatment significantly reduces the tumor progression. The body weights of mice in EC359-treated groups remains unchanged confirming the low toxicity of EC359[1].

Animal Model: 8-week-old female athymic nude mice with MDA-MB-231 cells[1]
Dosage: 5 mg/kg
Administration: Subcutaneous injection; 3 days per week; for 25 days
Result: Significantly reduced the tumor progression.
Molecular Weight

540.68

Formula

C₃₆H₃₈F₂O₂

CAS No.

2012591-09-0

SMILES

C[[email protected]@]12[[email protected]](O)(C(F)(F)C#C)CC[[email protected]@]1([H])[[email protected]]3([H])CCC4=CC(CCC4=C3[[email protected]@H](C5=CC=C(C6=C(C)C=C(C)C=C6C)C=C5)C2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

EC359EC 359EC-359ApoptosisInhibitorinhibitorinhibit

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