| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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Purity: ≥98%
NU6102 is a novel and potent inhibitor of Cdk1 and Cdk2 with Kis of 9 and 6 nM and IC50 of 9.5 and 5.4 nM, respectively. NU 6102 inhibits Cdk4 activity with an IC50 of 1.6 μM
| 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].
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| 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].
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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). |
| References |
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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.
Products are for research use only; We do not sell to patients
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