ETC-501
Based on 1 Customer Validation
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.
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- Purity: 97.40%
- CAS No.: 3094990-88-9
- 화학식: C26H24N6O2
- 분자량:452.51
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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.
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Cell Line:LN-229, T98G (human glioblastoma cell lines)
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Concentration:0, 0.1. 1, 2.5, 5, 10 and 20 μM
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Incubation Time:24 h
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Result:Caused a dose-dependent reduction in phosphorylation of eIF4E without altering total eIF4E protein levels.
Reduced Cyclin D1 protein levels.
| Species | Dose | Route | AUC | T1/2 |
|---|---|---|---|---|
| Mice[1] | 10 mg/kg | p.o. | 4.51 h | 3.84 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD-SCID gamma (NSG, NOD.Cg-PrkdcscidIl2rgtm1wjl/SzJ) (6-8-week-old male; subcutaneous glioblastoma model)[1]
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Dosage:100 mg/kg
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Administration:oral gavage; daily; 21 days
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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.
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Animal Model:NOD-SCID gamma (NSG, NOD.Cg-PrkdcscidIl2rgtm1wjl/SzJ) (6-8-week-old male; orthotopic intracranial glioblastoma model)[1]
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Dosage:100 mg/kg
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Administration:oral gavage; daily; 21 days
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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.
Chemical Information
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CAS No. 3094990-88-9
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Appearance Solid
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분자량 452.51
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화학식 C26H24N6O2
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Color Light yellow to green yellow
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SMILES
O=C(C1=CC=C(C2=NC3=C(C#CC4=CC=NC(N(C)C)=C4)C=NN3C=C2)C=C1)N5CCOCC5
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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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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