2. Apoptosis
  3. Apoptosis
  4. EC359

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. EC359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 416 In-stock
Solution
10 mM * 1 mL in DMSO USD 416 In-stock
Solid
5 mg USD 350 In-stock
10 mg USD 550 In-stock
50 mg USD 1650 In-stock
100 mg USD 2500 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 7 publication(s) in Google Scholar

EC359 Related Antibodies

Top Publications Citing Use of Products

    EC359 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2021 Feb 25;8(9):2003535.  [Abstract]

    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

    • Purity & Documentation

    • 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]. EC359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

    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].

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

    EC359 Related Antibodies

    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].

    MedChemExpress (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.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    C[C@@]12[C@](O)(C(F)(F)C#C)CC[C@@]1([H])[C@]3([H])CCC4=CC(CCC4=C3[C@@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 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (231.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    Volume (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

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

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (per animal)

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.8495 mL 9.2476 mL 18.4952 mL 46.2381 mL
    5 mM 0.3699 mL 1.8495 mL 3.6990 mL 9.2476 mL
    10 mM 0.1850 mL 0.9248 mL 1.8495 mL 4.6238 mL
    15 mM 0.1233 mL 0.6165 mL 1.2330 mL 3.0825 mL
    20 mM 0.0925 mL 0.4624 mL 0.9248 mL 2.3119 mL
    25 mM 0.0740 mL 0.3699 mL 0.7398 mL 1.8495 mL
    30 mM 0.0617 mL 0.3083 mL 0.6165 mL 1.5413 mL
    40 mM 0.0462 mL 0.2312 mL 0.4624 mL 1.1560 mL
    50 mM 0.0370 mL 0.1850 mL 0.3699 mL 0.9248 mL
    60 mM 0.0308 mL 0.1541 mL 0.3083 mL 0.7706 mL
    80 mM 0.0231 mL 0.1156 mL 0.2312 mL 0.5780 mL
    100 mM 0.0185 mL 0.0925 mL 0.1850 mL 0.4624 mL
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    EC359 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    EC3592012591-09-0EC 359EC-359ApoptosisInhibitorinhibitorinhibit

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