MRT00033659
Based on 1 Customer Validation
MRT00033659 is a potent broad-spectrum kinase inhibitor of CK1 (IC50=0.9 μM for CK1δ) and CHK1 (IC50=0.23 μM). MRT00033659, a pyrazolo-pyridine analogue, induces p53 pathway activation and E2F-1 destabilisation.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.40%
- No. CAS: 1401731-54-1
- Fòrmula: C15H14N4O
- Peso molecular:266.30
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years
* The compound is unstable in solutions, freshly prepared is recommended.
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
Actividad biológica
Descripciòn
IC50 & Target
[1]|
CK1δ 0.9 μM (IC50) |
Chk1 0.23 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
8 μM
Compound: MRT00033659
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Cytotoxicity against human A375 cells assessed as cell viability after 24 hrs by MTT assay
Cytotoxicity against human A375 cells assessed as cell viability after 24 hrs by MTT assay
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[PMID: 24007918] |
In Vitro
MRT00033659 (5-40 μM; 48 hours) is sufficient to significantly reduce cell number of 5 μM[1].
MRT00033659 (1-80 μM; 48 hours) induces substantial cell death from 5 μM[1].
MRT00033659 (0.2-80 μM; 48 hours) induces a robust and sustained stabilisation of p53, MDM2 and p21 proteins, as well as E2F-1 destabilisation from 0.2 μM to 5 μM[1].
MRT00033659 does not inhibit p38α MAPK[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:A375 cells
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Concentration:5, 20, 40 µM
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Incubation Time:48 hours
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Result:Significantly reduced cell number of 5 µM.
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Cell Line:A375 cells
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Concentration:1, 5, 10, 20, 40, 80 µM
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Incubation Time:48 hours
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Result:Induced substantial cell death from 5 µM.
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Cell Line:A375 cells
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Concentration:0.2, 1, 5, 10, 20, 40, 80 µM
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Incubation Time:48 hours
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Result:Induced a robust and sustained stabilisation of p53, MDM2 and p21 proteins, as well as E2F-1 destabilisation from 0.2 µM to 5 µM.
Chemical Information
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No. CAS 1401731-54-1
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Appearance Solid
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Peso molecular 266.30
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Fòrmula C15H14N4O
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Color Off-white to light yellow
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SMILES
CC1=NNC2=NC=C(C=C21)C3=CC=CC(NC(C)=O)=C3
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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 * The compound is unstable in solutions, freshly prepared is recommended.
Solvente y solubilidad
In Vitro:
DMSO : 83.33 mg/mL (312.92 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. The compound is unstable in solutions, freshly prepared is recommended.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
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: ≥ 4.17 mg/mL (15.66 mM); Clear solution
This protocol yields a clear solution of ≥ 4.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (41.7 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: ≥ 4.17 mg/mL (15.66 mM); Clear solution
This protocol yields a clear solution of ≥ 4.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (41.7 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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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. * The compound is unstable in solutions, freshly prepared is recommended.
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 (274 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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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.7552 mL | 18.7758 mL | 37.5516 mL | 93.8791 mL |
| 5 mM | 0.7510 mL | 3.7552 mL | 7.5103 mL | 18.7758 mL | |
| 10 mM | 0.3755 mL | 1.8776 mL | 3.7552 mL | 9.3879 mL | |
| 15 mM | 0.2503 mL | 1.2517 mL | 2.5034 mL | 6.2586 mL | |
| 20 mM | 0.1878 mL | 0.9388 mL | 1.8776 mL | 4.6940 mL | |
| 25 mM | 0.1502 mL | 0.7510 mL | 1.5021 mL | 3.7552 mL | |
| 30 mM | 0.1252 mL | 0.6259 mL | 1.2517 mL | 3.1293 mL | |
| 40 mM | 0.0939 mL | 0.4694 mL | 0.9388 mL | 2.3470 mL | |
| 50 mM | 0.0751 mL | 0.3755 mL | 0.7510 mL | 1.8776 mL | |
| 60 mM | 0.0626 mL | 0.3129 mL | 0.6259 mL | 1.5647 mL | |
| 80 mM | 0.0469 mL | 0.2347 mL | 0.4694 mL | 1.1735 mL | |
| 100 mM | 0.0376 mL | 0.1878 mL | 0.3755 mL | 0.9388 mL |
MRT00033659 Related Classifications
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