CK2 inhibitor 2
Based on 1 Customer Validation
CK2 inhibitor 2 is a potent, selective and orally active inhibitor of CK2, with an IC50 of 0.66 nM. CK2 inhibitor 2 shows high selectivity for Clk2 (IC50=32.69 nM)/CK2. CK2 inhibitor 2 exhibits favorable antiproliferative and antitumor activity.
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- Pureza: 98.51%
- No. CAS: 2641079-92-5
- Fòrmula: C21H17ClN4O2
- Peso molecular:392.84
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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Actividad biológica
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CK2 0.66 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
3.07 μM
Compound: 1c
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Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 33834781] |
| HT-29 | IC50 |
5.18 μM
Compound: 1c
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Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 33834781] |
| L02 | IC50 |
96.68 μM
Compound: 1c
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Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 33834781] |
| MCF7 | IC50 |
7.5 μM
Compound: 1c
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Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 33834781] |
| PC-3 | IC50 |
4.53 μM
Compound: 1c
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Cytotoxicity against human PC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human PC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 33834781] |
| T-24 | IC50 |
6.1 μM
Compound: 1c
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Cytotoxicity against human T24 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human T24 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 33834781] |
CK2 inhibitor 2 (compound 1c) exhibits potent antiproliferative activities against PC-3, HCT-116, MCF-7, HT-29, T24 and LO2 cells, with IC50s of 4.53 μM, 3.07 μM, 7.50 μM, 5.18 μM, 6.10 μM, and 96.68 μM, respectively[1].
CK2 inhibitor 2 (5-20 μM; 24 h) induces apoptosis of HCT-116 cells in a dose-dependent manner. CK2 inhibitor 2 dose-dependently suppresses the expression of p-Akt1S129 and p-Cdc37S13 in HCT-116 cells[1].
CK2 inhibitor 2 (1-500 nM) dose-dependently inhibits exogenous ALDH1A1 enzyme activity, with an IC50 of 0.10 μM[1].
CK2 inhibitor 2 (5-20 μM; 24 h) inhibits the transcription and protein expression of ALDH1A1 in HCT-116 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116 cells
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Concentration:5, 10, 20 μM
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Incubation Time:24 hours
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Result:The apoptotic ratio reached about 55% at the concentration of 20 μM.
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Cell Line:HCT-116 cells
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Concentration:5, 10, 20 μM
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Incubation Time:24 hours
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Result:Inhibited the expression of p-Akt1S129 and p-Cdc37S13 in a dose-dependent manner.
CK2 inhibitor 2 (25 mg/kg; a single p.o.) exhibits Cmax (7017.8 ng/mL), elimination half-life (t1/2=6.67 h), and CL (0.60 L/h/kg) in SD rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BALB/c athymic nude mice (5 weeks old; 16-18 g) were injected HCT-116 cells[1]
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Dosage:60, 90 mg/kg
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Administration:P.o. twice a day for 4 weeks
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Result:Inhibited the tumor growth in a dose-dependent manner.
No conspicuous change in body weight.
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Animal Model:Sprague-Dawley (SD) rats[1]
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Dosage:25 mg/kg (Pharmacokinetic Analysis)
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Administration:A single p.o.
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Result:Cmax=7017.8 ng/mL, t1/2=6.67 h, CL=0.60 L/h/kg.
Chemical Information
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No. CAS 2641079-92-5
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Appearance Solid
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Peso molecular 392.84
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Fòrmula C21H17ClN4O2
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Color White to yellow
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SMILES
O=C(C1=CC2=C(C3=CN=CC=C3C(NC4=CC(Cl)=CC=C4)=N2)C=C1)NCCO
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 50 mg/mL (127.28 mM; ultrasonic and warming and heat to 60°C; 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)
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.
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 (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 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 | 2.5456 mL | 12.7278 mL | 25.4557 mL | 63.6391 mL |
| 5 mM | 0.5091 mL | 2.5456 mL | 5.0911 mL | 12.7278 mL | |
| 10 mM | 0.2546 mL | 1.2728 mL | 2.5456 mL | 6.3639 mL | |
| 15 mM | 0.1697 mL | 0.8485 mL | 1.6970 mL | 4.2426 mL | |
| 20 mM | 0.1273 mL | 0.6364 mL | 1.2728 mL | 3.1820 mL | |
| 25 mM | 0.1018 mL | 0.5091 mL | 1.0182 mL | 2.5456 mL | |
| 30 mM | 0.0849 mL | 0.4243 mL | 0.8485 mL | 2.1213 mL | |
| 40 mM | 0.0636 mL | 0.3182 mL | 0.6364 mL | 1.5910 mL | |
| 50 mM | 0.0509 mL | 0.2546 mL | 0.5091 mL | 1.2728 mL | |
| 60 mM | 0.0424 mL | 0.2121 mL | 0.4243 mL | 1.0607 mL | |
| 80 mM | 0.0318 mL | 0.1591 mL | 0.3182 mL | 0.7955 mL | |
| 100 mM | 0.0255 mL | 0.1273 mL | 0.2546 mL | 0.6364 mL |
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