| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
NU6102 targets CDK1/cyclin B and CDK2/cyclin A3 with IC50 values of 9.5 nM and 5.4 nM, respectively. It 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).
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| ln Vitro |
NU6102 selectively inhibits the growth of CDK2 WT (wild type) and KO MEF (knockout mouse embryonic fibroblasts) (GI50 of 14 μM and >30 μM). Treatment with NU6102 (0-30 μM; 1-24 hours; SKUT 1B cells) induces G2 arrest, inhibition of Rb phosphorylation, and cytotoxicity in SKUT-1B cells (LC50 after 24 hours of exposure is 2.6 μM) [3]. NU6102 inhibits cell growth and causes cell cycle phase arrest in a time-dependent manner in human breast cancer cell lines, G2/M phase arrest in asynchronously growing cell lines, cells released by serum starvation, and G1 in the nucleus of Xenopus laevis cells /S phase arrest[3].
In vitro, NU6102 is a potent inhibitor of CDK1 and CDK2. It inhibits cell growth. It is 1,000-fold more potent than NU2058. It inhibits Cdk4 activity with an IC50 of 1.6 μM. |
| ln Vivo |
After administering NU6102 intravenously and intraperitoneally to Balb/C mice, the drug's pharmacokinetics were ascertained. The maximum dosing dose of NU6102 is 1 mg/kg iv and 10 mg/kg ip due to its limited solubility. NU6301 releases NU6102 after ip or iv administration, and peak plasma levels of 12 μM NU6102 are observed 5 minutes after iv administration. The peak concentration reached after intravenous injection of the maximum dose of NU6102 was 0.92 μM. Following the injection of NU6301, the plasma half-life of NU6102 is 42 minutes for intraperitoneal administration and 10 minutes for intravenous administration [3].
In vivo, NU6102 has demonstrated antiproliferative properties. It is used as a research tool to study cell cycle regulation and CDK function. Detailed in vivo studies are limited, as the compound is primarily used for in vitro research. |
| Enzyme Assay |
In vitro enzyme assays for NU6102 typically measure its ability to inhibit CDK1/cyclin B and CDK2/cyclin A3 kinase activity. The enzyme is incubated with a peptide substrate and ATP in the presence of increasing concentrations of the compound. Phosphorylation is detected using radioactive or fluorescence-based methods. IC50 and Ki values are calculated.
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| Cell Assay |
Cell cycle analysis[3]
Cell Types: SKUT 1B Cell Tested Concentrations: 0 μM, 3 μM, 10 μM and 30 μM Incubation Duration: 1 hour, 3 hrs (hours), 6 hrs (hours) and 24 hrs (hours) Experimental Results: Induction of G2 arrest, inhibition of Rb phosphorylation and cytotoxicity (LC50 2.6 μM after 24 hrs (hours) of exposure). Cell-based assays for NU6102 involve treating various cancer cell lines with the compound and measuring cell proliferation, cell cycle distribution, and apoptosis. Cell viability is assessed using MTT assays. Cell cycle analysis is performed by flow cytometry. The compound's antiproliferative effects are quantified. |
| Animal Protocol |
In vivo animal studies for NU6102 are limited. The compound is primarily used in vitro. When used in animal models, it is typically administered to tumor-bearing mice to assess its antitumor efficacy. Tumor growth inhibition and survival are evaluated.
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| ADME/Pharmacokinetics |
Dedicated pharmacokinetic data for NU6102 is limited. The compound has a molecular weight of 389.43 g/mol and a molecular formula of C18H19N7O3S. It is a cell-permeable purine analog. Its absorption, distribution, metabolism, and excretion have not been extensively studied.
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| Toxicity/Toxicokinetics |
The toxicological profile of NU6102 has not been extensively characterized. As a research compound, it should be handled with appropriate safety precautions. Its antiproliferative properties suggest potential cytotoxicity.
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| References |
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| Additional Infomation |
NU6102 is a potent and ATP-competitive inhibitor of CDK1 and CDK2. It is a valuable research tool for studying cell cycle regulation, CDK function, and cancer biology. It is not approved for therapeutic use. It is also known as Cdk1/2 Inhibitor II.
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| Molecular Formula |
C18H22N6O3S
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|---|---|
| Molecular Weight |
402.47068
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| Exact Mass |
402.147
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| CAS # |
444722-95-6
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| PubChem CID |
4566
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| Appearance |
White to yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
612.9±65.0 °C at 760 mmHg
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| Flash Point |
324.5±34.3 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.746
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| LogP |
1.42
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
601
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
OWXORKPNCHJYOF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H22N6O3S/c19-28(25,26)14-8-6-13(7-9-14)22-18-23-16-15(20-11-21-16)17(24-18)27-10-12-4-2-1-3-5-12/h6-9,11-12H,1-5,10H2,(H2,19,25,26)(H2,20,21,22,23,24)
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| Chemical Name |
4-((6-(cyclohexylmethoxy)-9H-purin-2-yl)amino)benzenesulfonamide
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| Synonyms |
NU6102 NU-6102 NU 6102.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~248.47 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.21 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4847 mL | 12.4233 mL | 24.8466 mL | |
| 5 mM | 0.4969 mL | 2.4847 mL | 4.9693 mL | |
| 10 mM | 0.2485 mL | 1.2423 mL | 2.4847 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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