NU6102
Based on 1 Customer Validation
NU6102 is a potent CDK1 and CDK2 inhibitor with IC50s of 9.5 nM and 5.4 nM for CDK1/cyclinB and CDK2/cyclinA3, respectively. NU6102 shows selectivity for CDK1/CDK2 over CDK4 (IC50 of 1.6 μM), DYRK1A (IC50 of 0.9 μM), PDK1 (IC50 of 0.8 μM) and ROCKII (IC50 of 0.6 μM).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.23%
- No. CAS: 444722-95-6
- Fòrmula: C18H22N6O3S
- Peso molecular:402.47
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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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Actividad biológica
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Cdk1/cyclin B 9.5 nM (IC50) |
CDK2/cyclin A3 5.4 nM (IC50) |
CDK4 1.6 μM (IC50) |
DYRK1A 0.9 μM (IC50) |
PDK1 0.8 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
0.022 μM
Compound: NU6102
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Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
0.117 μM
Compound: NU6102
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Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
0.146 μM
Compound: NU6102
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Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
0.184 μM
Compound: NU6102
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Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
2.5 μM
Compound: NU6102
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Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
4.1 μM
Compound: NU6102
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Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
NU6102 (0-30 μM; 1-24 hours; SKUT 1B cells) treatment induces a G2 arrest, inhibition of Rb phosphorylation and cytotoxicity (LC50 2.6 μM for a 24 h exposure) in SKUT-1B cells[3].
NU6102 inhibits cell growth and causes cell cycle phase arrest in human breast cancer cell lines, G2/M arrest in asynchronously growing cell lines and G1/S arrest in cells released from serum starvation, and in Xenopus nuclei in a timedependent manner[3].
NU6102 selectively inhibits the growth of CDK2 WT (wild type) versus KO MEFs (knockout mouse embryo fibroblasts) (GI50 of 14 μM versus >30 μM)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SKUT 1B cells
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Concentration:0 μM, 3 μM, 10 μM, and 30 μM
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Incubation Time:1 hours, 3 hours, 6 hours, and 24 hours
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Result:Induced a G2 arrest, inhibition of Rb phosphorylation and cytotoxicity (LC50 2.6 μM for a 24 h exposure).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 444722-95-6
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Appearance Solid
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Peso molecular 402.47
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Fòrmula C18H22N6O3S
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Color White to yellow
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SMILES
O=S(C1=CC=C(NC2=NC(OCC3CCCCC3)=C4N=CNC4=N2)C=C1)(N)=O
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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
DMSO : 100 mg/mL (248.47 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)
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 (6.21 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 (6.21 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 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.
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 (278 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Ian R Hardcastle, et al. N2-substituted O6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2. J Med Chem. 2004 Jul 15;47(15):3710-22. [Content Brief]
[2]. David J Pratt, et al. Dissecting the determinants of cyclin-dependent kinase 2 and cyclin-dependent kinase 4 inhibitor selectivity. J Med Chem. 2006 Sep 7;49(18):5470-7. [Content Brief]
[3]. Huw D Thomas , et al. Preclinical in vitro and in vivo evaluation of the potent and specific cyclin-dependent kinase 2 inhibitor NU6102 and a water soluble prodrug NU6301. Eur J Cancer. 2011 Sep;47(13):2052-9. [Content Brief]
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 | 2.4847 mL | 12.4233 mL | 24.8466 mL | 62.1164 mL |
| 5 mM | 0.4969 mL | 2.4847 mL | 4.9693 mL | 12.4233 mL | |
| 10 mM | 0.2485 mL | 1.2423 mL | 2.4847 mL | 6.2116 mL | |
| 15 mM | 0.1656 mL | 0.8282 mL | 1.6564 mL | 4.1411 mL | |
| 20 mM | 0.1242 mL | 0.6212 mL | 1.2423 mL | 3.1058 mL | |
| 25 mM | 0.0994 mL | 0.4969 mL | 0.9939 mL | 2.4847 mL | |
| 30 mM | 0.0828 mL | 0.4141 mL | 0.8282 mL | 2.0705 mL | |
| 40 mM | 0.0621 mL | 0.3106 mL | 0.6212 mL | 1.5529 mL | |
| 50 mM | 0.0497 mL | 0.2485 mL | 0.4969 mL | 1.2423 mL | |
| 60 mM | 0.0414 mL | 0.2071 mL | 0.4141 mL | 1.0353 mL | |
| 80 mM | 0.0311 mL | 0.1553 mL | 0.3106 mL | 0.7765 mL | |
| 100 mM | 0.0248 mL | 0.1242 mL | 0.2485 mL | 0.6212 mL |
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