Referencia número: HY-120142

EC359

11 Cited Publications

Revisión del cliente

Based on 11 publication(s) in Google Scholar

EC359 is a potent, selective, high affinity and orally active leukemia inhibitory factor receptor (LIFR) inhibitor with a K_d 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.

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Pureza: 99.77%
No. CAS: 2012591-09-0
Fòrmula: C₃₆H₃₈F₂O₂
Peso molecular:540.68

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

EC359 Chemical Structure

No. CAS: 2012591-09-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (11)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

EC359 is a potent, selective, high affinity and orally active leukemia inhibitory factor receptor (LIFR) inhibitor with a K_d 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.

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.

Chemical Information

No. CAS 2012591-09-0
Appearance Solid
Peso molecular 540.68
Fòrmula C₃₆H₃₈F₂O₂
Color Off-white 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
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (11)

All Histological Imaging/StainingFlow CytometryWBCell Proliferation/Viability AssayCell Imaging/Staining

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Journal Impact Factor

J Clin Invest

Neuroprotection against ischemic stroke requires a specific class of early responder T cells in mice. [Abstract]

2022 Aug 1;132(15):e157678. PMID: 35912857

EC359 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2022 Aug 1;132(15):e157678. [Abstract]

Spleen-derived CD8+ TRLs were pretreated with EC359 (LIFR inhibitor, 100 nM) for 1 hour and then injected (i.v., 1 × 10⁶ cells into recipient mice 2 hours after tMCAO. LIF treatment enhanced ETGF and IL-10 expression in CD8+ TRLs. n = 3/group.

EC359 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2022 Aug 1;132(15):e157678. [Abstract]

Spleen-derived CD8+ TRLs were pretreated with EC359 (LIFR inhibitor, 100 nM) for 1 hour and then injected (i.v., 1 × 10⁶ cells into recipient mice 2 hours after tMCAO. Quantification of MAP2 staining and Garcia score. n = 5–6/group.
Adv Sci (Weinh)

p16Ink4a-Positive Hepatocytes Drive Liver Fibrosis Through Activation of LIFR Family Pathway. [Abstract]

2026 Jan 25:e10562. PMID: 41580988

EC359 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2026 Jan 25:e10562. [Abstract]

Sirius red staining results of the liver following 4‐week treatment of CCl4 with vehicle or 5 mg/kgBW of EC359. The representative images were shown in the left panel. Scale bar, 500 µm.
Adv Sci (Weinh)

SNORA28 Promotes Proliferation and Radioresistance in Colorectal Cancer Cells through the STAT3 Pathway by Increasing H3K9 Acetylation in the LIFR Promoter. [Abstract]

2024 Jun 26:e2405332. PMID: 38924373

EC359 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun 26:e2405332. [Abstract]

Western blotting analysis of the indicated proteins in SNORA28 overexpressing CRC cells treated with 5 µM EC359 for 24 h.

EC359 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun 26:e2405332. [Abstract]

CCK8 analyses of the proliferation (n = 5) and survival ability (n = 3) in SNORA28 overexpressing CRC cells treated with 5 µM EC359 for 24 h.

EC359 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun 26:e2405332. [Abstract]

Colony formation analyses of the proliferation (n = 5) and survival ability (n = 3) in SNORA28 overexpressing CRC cells treated with 5 µM EC359 for 24 h.
Adv Sci (Weinh)

MgFe-LDH Nanoparticles: A Promising Leukemia Inhibitory Factor Replacement for Self-Renewal and Pluripotency Maintenance in Cultured Mouse Embryonic Stem Cells. [Abstract]

2021 Feb 25;8(9):2003535. PMID: 33977050

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.
Cells

Repositioning Mifepristone as a Leukaemia Inhibitory Factor Receptor Antagonist for the Treatment of Pancreatic Adenocarcinoma. [Abstract]

2022 Nov 3;11(21):3482. PMID: 36359879
Eur J Pharmacol

Leukemia inhibitory factor receptor inhibition by EC359 reduces atherosclerotic stenosis grade in Ldlr-/- mice. [Abstract]

2024 Nov 9:177121. PMID: 39528103
Sci Rep

Stromal transcriptomics uncover LIF as a key effector in high tumor budding triple-negative breast cancer. [Abstract]

2025 Nov 25. PMID: 41290930
Cancers (Basel)

Heterogeneity in the Metastatic Microenvironment: JunB-Expressing Microglia Cells as Potential Drivers of Melanoma Brain Metastasis Progression. [Abstract]

2023 Oct 13;15(20):4979. PMID: 37894348
Endocrinology

Human seminal extracellular vesicles enhance endometrial receptivity through leukemia inhibitory factor. [Abstract]

2024 Mar 29;165(5):bqae035. PMID: 38518755
bioRxiv

Targeting CREB remodels the immune microenvironment to enhance immunotherapy responses in pancreatic cancer. [Abstract]

2025 Dec 8:2025.12.04.691935. PMID: 41394608
bioRxiv

2023 Oct 2.

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (184.95 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: 0.5% CMC-Na/0.5% Tween-80 in Saline water

Solubility: 4.98 mg/mL (9.21 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (282 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

EC359

11 Cited Publications

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EC359

Apoptosis Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Alkyne Compound Library

Publications Citing Use of MedChemExpress (MCE) EC359

Actividad biológica

Chemical Information

Publications (11)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

EC359

Apoptosis Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Alkyne Compound Library

Publications Citing Use of MedChemExpress (MCE) EC359

Actividad biológica

Chemical Information

Publications (11)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

EC359 Related Classifications

HY-120142 Related Classifications