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EC359 

Cat. No.: HY-120142 Purity: 99.24%
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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 416 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2500 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE EC359

    EC359 purchased from MCE. Usage Cited in: Adv Sci. 2021 Feb 25.

    Western blot is applied to measure protein expression changes in mESCs cultured for 3 d on gelatin, with or without EC359 (150 μM). Addition of EC359 significantly decreases the LIFR-mediated activation of p-STAT3 and phospho-protein kinase B (p-AKT) whereas increased phospho-extracellular signal-regulated kinase (p-ERK) expression in the LIF+ group.
    • Biological Activity

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    • References

    • Customer Review

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (231.19 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8495 mL 9.2476 mL 18.4952 mL
    5 mM 0.3699 mL 1.8495 mL 3.6990 mL
    10 mM 0.1850 mL 0.9248 mL 1.8495 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (3.85 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (3.85 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.24%

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    Keywords:

    EC359EC 359EC-359ApoptosisInhibitorinhibitorinhibit

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