MK-8353
Based on 5 publication(s) in Google Scholar
MK-8353 (SCH900353) is a potent, selective and orally available ERK1/2 inhibitor, with IC50s of 23.0 nM and 8.8 nM, respectively; MK-8353 has antitumor activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.13%
- No. CAS: 1184173-73-6
- Fòrmula: C37H41N9O3S
- Peso molecular:691.84
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) MK-8353
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Customer Validation & Images
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
ERK2 8.8 nM (IC50) |
ERK1 23 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2058 | IC50 |
371 nM
Compound: 20; MK-8353
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Antiproliferative activity against human A2058 cells harboring BRAF V600E/D mutant measured after 4 days
Antiproliferative activity against human A2058 cells harboring BRAF V600E/D mutant measured after 4 days
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[PMID: 30034615] |
| COLO 205 | IC50 |
23 nM
Compound: 20; MK-8353
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Antiproliferative activity against human COLO205 cells harboring BRAF V600E/D mutant measured after 4 days
Antiproliferative activity against human COLO205 cells harboring BRAF V600E/D mutant measured after 4 days
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[PMID: 30034615] |
| HT-29 | IC50 |
51 nM
Compound: 20; MK-8353
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Antiproliferative activity against human HT-29 cells harboring BRAF V600E/D mutant measured after 4 days
Antiproliferative activity against human HT-29 cells harboring BRAF V600E/D mutant measured after 4 days
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[PMID: 30034615] |
In Vitro
MK-8353 is a potent, selective and orally available ERK1/2 inhibitor, with IC50s of 23.0 nM and 8.8 nM, respectively; MK-8353 has antitumor activity. MK-8353 only at 1 μM shows >50% inhibition on 3 kinases (CLK2, FLT4, and Aurora B), and no other kinases tested are inhibited by >35% at 0.1 μM. MK-8353 also shows potent antitumor activity against various cancer cell lines, such Malme-3M cells (Melanoma), Colo-205 cells (Colon), NCI-H292 cells (Lung), A-549 cells (NSCLC), 8505C cells (Thyroid), SW-626 cells (Ovarian), with EC50s of 21 nM, 19 nM, 130 nM, 230 nM, 210 nM, 108 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1184173-73-6
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Appearance Solid
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Peso molecular 691.84
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Fòrmula C37H41N9O3S
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Color White to light yellow
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SMILES
O=C([C@@]1(SC)CN(CC(N2CC=C(C3=CC=C(C4=NN(C)C=N4)C=C3)CC2)=O)CC1)NC5=CC6=C(NN=C6C7=CC=C(OC(C)C)N=C7)C=C5
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Synonyms
SCH900353
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (5)
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Journal Impact Factor
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Most Recent
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Nat Nanotechnol
Therapeutically reprogrammed nutrient signalling enhances nanoparticulate albumin bound drug uptake and efficacy in KRAS-mutant cancer. [Abstract]2021 Jul;16(7):830-839. PMID: 33958764 -
J Nanobiotechnology
Delivery of an ERK inhibitor using bioactive lipid nanoparticles reduces angiogenesis and prevents oral squamous cell carcinoma development. [Abstract]2025 Jul 18;23(1):524. PMID: 40682120 -
Cell Rep
2024 Dec 3;43(12):115026. PMID: 39630579 -
Mol Med Rep
S100A1 expression is increased in spinal cord injury and promotes inflammation, oxidative stress and apoptosis of PC12 cells induced by LPS via ERK signaling. [Abstract]2023 Feb;27(2):30. PMID: 36524376
MK-8353 purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2023 Feb;27(2):30. [Abstract]
MK‑8353 partially counteractes the inhibitory effects of S100A1 overexpression on Nrf2 level in PC12 cells.
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Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (144.54 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. 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. 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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.01 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.
In Vivo Dissolution Calculator
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.
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.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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. 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 | 1.4454 mL | 7.2271 mL | 14.4542 mL | 36.1355 mL |
| 5 mM | 0.2891 mL | 1.4454 mL | 2.8908 mL | 7.2271 mL | |
| 10 mM | 0.1445 mL | 0.7227 mL | 1.4454 mL | 3.6136 mL | |
| 15 mM | 0.0964 mL | 0.4818 mL | 0.9636 mL | 2.4090 mL | |
| 20 mM | 0.0723 mL | 0.3614 mL | 0.7227 mL | 1.8068 mL | |
| 25 mM | 0.0578 mL | 0.2891 mL | 0.5782 mL | 1.4454 mL | |
| 30 mM | 0.0482 mL | 0.2409 mL | 0.4818 mL | 1.2045 mL | |
| 40 mM | 0.0361 mL | 0.1807 mL | 0.3614 mL | 0.9034 mL | |
| 50 mM | 0.0289 mL | 0.1445 mL | 0.2891 mL | 0.7227 mL | |
| 60 mM | 0.0241 mL | 0.1205 mL | 0.2409 mL | 0.6023 mL | |
| 80 mM | 0.0181 mL | 0.0903 mL | 0.1807 mL | 0.4517 mL | |
| 100 mM | 0.0145 mL | 0.0723 mL | 0.1445 mL | 0.3614 mL |
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