2. MAPK/ERK Pathway Cell Cycle/DNA Damage Immunology/Inflammation
  3. MNK DNA/RNA Synthesis Interleukin Related Eukaryotic Initiation Factor (eIF)
  4. ETC-501

ETC-501 is a blood-brain barrier-permeable, orally active, and selective MNK1/MNK2 inhibitor, with an IC50 of 0.033 μM against MNK1 and 0.111 μM against MNK2. ETC-501 inhibits glioblastoma cell proliferation, impairs DNA damage repair function, delays cell cycle progression, and suppresses ribosome biogenesis. ETC-501 enhances Temozolomide (HY-17364)-induced cellular senescence, attenuates the senescence-associated secretory phenotype, and increases cellular sensitivity to Navitoclax (HY-10087). ETC-501 is applicable to research related to glioblastoma.

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

ETC-501

ETC-501 Chemical Structure

CAS No. : 3094990-88-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
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25 mg In-stock
50 mg In-stock
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ETC-501 Related Antibodies

Top Publications Citing Use of Products

View All MNK Isoform Specific Products:

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MNK1 MNK2 MNK

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

ETC-501 is a blood-brain barrier-permeable, orally active, and selective MNK1/MNK2 inhibitor, with an IC50 of 0.033 μM against MNK1 and 0.111 μM against MNK2. ETC-501 inhibits glioblastoma cell proliferation, impairs DNA damage repair function, delays cell cycle progression, and suppresses ribosome biogenesis. ETC-501 enhances Temozolomide (HY-17364)-induced cellular senescence, attenuates the senescence-associated secretory phenotype, and increases cellular sensitivity to Navitoclax (HY-10087). ETC-501 is applicable to research related to glioblastoma[1].

In Vitro

ETC-501 (0-20 μM; 24 h) dose-dependently inhibits eIF4E phosphorylation and reduces Cyclin D1 protein levels in LN-229 and T98G glioblastoma cells[1].
ETC-501 (0-10 μM) inhibits the viability of LN-229 and T98G glioblastoma cells with GI50 values of 4.035 μM and 6.122 μM, respectively, and reduces the tumor sphere-forming capacity and stem cell frequency of patient-derived GPCs[1].
ETC-501 (0-10 μM; 4 h) impairs DNA synthesis in LN-229, T98G and U-87MG glioblastoma cells in a dose-dependent manner[1].
ETC-501 (8 h) impairs G1-to-S phase progression in Palbociclib (HY-50767)-synchronized LN-229 and U-87MG glioblastoma cells[1].
ETC-501 (5-10 μM; 14 days) induces cellular senescence in LN-229 and U-87MG glioblastoma cells[1].
ETC-501 (5-10 μM; 10 days) reduces the levels of key inflammatory cytokines and chemokines, including IL-6, IL-8 and CCL2[1].
ETC-501 (10 μM; 6 days) and TMZ (HY-17364) drives LN-229 glioblastoma cells into a senescence priming state, and significantly enhances their sensitivity to Navitoclax (HY-10087)-induced cell death and apoptosis[1].

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

ETC-501 Related Antibodies

Western Blot Analysis[1]

Cell Line: LN-229, T98G (human glioblastoma cell lines)
Concentration: 0, 0.1. 1, 2.5, 5, 10 and 20 μM
Incubation Time: 24 h
Result: Caused a dose-dependent reduction in phosphorylation of eIF4E without altering total eIF4E protein levels.
Reduced Cyclin D1 protein levels.
Parmacokinetics
Species Dose Route AUC T1/2
Mice[1] 10 mg/kg p.o. 4.51 h 3.84 h
In Vivo

ETC-501 (100 mg/kg; oral gavage; once daily; 21 days) enhances tumor cell senescence and attenuates the senescence-associated secretory phenotype when combined with TMZ (HY-17364) in NSG mice bearing orthotopic or subcutaneous glioblastoma, and the additional combination with Navitoclax (HY-10087) effectively eliminates senescent cells[1].

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

Animal Model: NOD-SCID gamma (NSG, NOD.Cg-PrkdcscidIl2rgtm1wjl/SzJ) (6-8-week-old male; subcutaneous glioblastoma model)[1]
Dosage: 100 mg/kg
Administration: oral gavage; daily; 21 days
Result: Reduced excised tumor p-eIF4E levels by ~50%.
Induced senescent tumor cells (SA-β-gal positive) when combined with TMZ, with non-statistically significant trend toward higher SA-β-gal and p21 levels compared to TMZ alone.
Resulted in widespread tumor necrosis, near absence of SA-β-gal-positive cells, and markedly reduced p21 expression when combined with TMZ and navitoclax.
Animal Model: NOD-SCID gamma (NSG, NOD.Cg-PrkdcscidIl2rgtm1wjl/SzJ) (6-8-week-old male; orthotopic intracranial glioblastoma model)[1]
Dosage: 100 mg/kg
Administration: oral gavage; daily; 21 days
Result: Reduced p-eIF4E levels in contralateral and ipsilateral brain tissue by ~60%.
Did not significantly extend survival compared to vehicle control when administered alone.
Showed non-statistically significant trend toward improved survival compared to TMZ alone, and induced senescence (SA-β-gal positive) in orthotopic tumors when combined with TMZ.
Did not improve survival beyond TMZ alone when combined with TMZ and navitoclax, with residual SA-β-gal-positive senescent cells detected post-treatment.
Molecular Weight

452.51

Formula

C26H24N6O2
CAS No.
Appearance

Solid

SMILES

O=C(C1=CC=C(C2=NC3=C(C#CC4=CC=NC(N(C)C)=C4)C=NN3C=C2)C=C1)N5CCOCC5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (110.49 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 2.2099 mL 11.0495 mL 22.0990 mL
5 mM 0.4420 mL 2.2099 mL 4.4198 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.5 mg/mL (5.52 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.52 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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

Purity: 97.40%

COA (253 KB)

Handling Instructions (2659 KB)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2099 mL 11.0495 mL 22.0990 mL 55.2474 mL
5 mM 0.4420 mL 2.2099 mL 4.4198 mL 11.0495 mL
10 mM 0.2210 mL 1.1049 mL 2.2099 mL 5.5247 mL
15 mM 0.1473 mL 0.7366 mL 1.4733 mL 3.6832 mL
20 mM 0.1105 mL 0.5525 mL 1.1049 mL 2.7624 mL
25 mM 0.0884 mL 0.4420 mL 0.8840 mL 2.2099 mL
30 mM 0.0737 mL 0.3683 mL 0.7366 mL 1.8416 mL
40 mM 0.0552 mL 0.2762 mL 0.5525 mL 1.3812 mL
50 mM 0.0442 mL 0.2210 mL 0.4420 mL 1.1049 mL
60 mM 0.0368 mL 0.1842 mL 0.3683 mL 0.9208 mL
80 mM 0.0276 mL 0.1381 mL 0.2762 mL 0.6906 mL
100 mM 0.0221 mL 0.1105 mL 0.2210 mL 0.5525 mL
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ETC-501 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:

ETC-5013094990-88-9ETC501ETC 501MNKDNA/RNA SynthesisInterleukin RelatedEukaryotic Initiation Factor (eIF)Mitogen activated protein kinase interacting kinaseMAP kinase interacting kinaseMAPK interacting kinaseILMNK2ribosome biogenesistemozolomidecell cycle regulationMNK1glioblastoma cellsDNA damage repairMYC signalinginflammationDNA replicationInhibitorinhibitorinhibit

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