PNU-292137
Based on 1 Customer Validation
PNU-292137 is an orally active, potent CDK2 inhibitor with IC50s of 37 nM and 92 nM for CDK2/cyclin A and CDK2/cyclin E, respectively. PNU-292137 makes interactions with the hydrophobic pocket at the back of the CDK2 ATP pocket. PNU-292137 efficiently inhibits tumor cell proliferation in human colon and prostate tumor cell lines. PNU-292137 exhibits antitumor activity (TGI>50%) in a mouse xenograft model.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.95%
- No. CAS: 326823-27-2
- Fòrmula: C18H17N3O
- Peso molecular:291.35
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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
Actividad biológica
Descripciòn
IC50 & Target
[1]|
CDK2/cyclinA 37 nM (IC50) |
CDK2/cyclin E 92 nM (IC50) |
Cdk5/p25 114 nM (IC50) |
CDK1/cyclinB 270 nM (IC50) |
CDK4/cyclinD1 >10000 nM (IC50) |
GSK-3β 1905 nM (IC50) |
ERK-2 4600 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
286 nM
Compound: 41
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Antiproliferative activity against human A2780 cells
Antiproliferative activity against human A2780 cells
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[PMID: 15189033] |
| A2780 | IC50 |
286 nM
Compound: 54(table 2)
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Inhibitory concentration towards human ovarian carcinoma cell line A2780
Inhibitory concentration towards human ovarian carcinoma cell line A2780
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[PMID: 15828833] |
| DU-145 | IC50 |
651 nM
Compound: 41
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Inhibition of human DU145 cell proliferation
Inhibition of human DU145 cell proliferation
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[PMID: 15189033] |
| HCT-116 | IC50 |
73 nM
Compound: 41
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Inhibition of human HCT116 cell proliferation
Inhibition of human HCT116 cell proliferation
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[PMID: 15189033] |
| HT-29 | IC50 |
170 nM
Compound: 41
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Inhibition of human H-29 cell proliferation
Inhibition of human H-29 cell proliferation
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[PMID: 15189033] |
Chemical Information
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No. CAS 326823-27-2
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Appearance Solid
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Peso molecular 291.35
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Fòrmula C18H17N3O
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Color White to off-white
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SMILES
O=C(CC1=CC=C2C=CC=CC2=C1)NC3=NNC(C4CC4)=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 In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (343.23 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: ≥ 2.5 mg/mL (8.58 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.
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 (271 KB)
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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)
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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 | 3.4323 mL | 17.1615 mL | 34.3230 mL | 85.8074 mL |
| 5 mM | 0.6865 mL | 3.4323 mL | 6.8646 mL | 17.1615 mL | |
| 10 mM | 0.3432 mL | 1.7161 mL | 3.4323 mL | 8.5807 mL | |
| 15 mM | 0.2288 mL | 1.1441 mL | 2.2882 mL | 5.7205 mL | |
| 20 mM | 0.1716 mL | 0.8581 mL | 1.7161 mL | 4.2904 mL | |
| 25 mM | 0.1373 mL | 0.6865 mL | 1.3729 mL | 3.4323 mL | |
| 30 mM | 0.1144 mL | 0.5720 mL | 1.1441 mL | 2.8602 mL | |
| 40 mM | 0.0858 mL | 0.4290 mL | 0.8581 mL | 2.1452 mL | |
| 50 mM | 0.0686 mL | 0.3432 mL | 0.6865 mL | 1.7161 mL | |
| 60 mM | 0.0572 mL | 0.2860 mL | 0.5720 mL | 1.4301 mL | |
| 80 mM | 0.0429 mL | 0.2145 mL | 0.4290 mL | 1.0726 mL | |
| 100 mM | 0.0343 mL | 0.1716 mL | 0.3432 mL | 0.8581 mL |
PNU-292137 Related Classifications
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