- NU 2058
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- $1.00 / 1g
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2020-01-15
- CAS:161058-83-9
- Min. Order: 1g
- Purity: 99%
- Supply Ability: 1000KGS
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| | NU 2058 Basic information |
| Product Name: | NU 2058 | | Synonyms: | CS-2601;NU 2058;NU-2058;NU2058;6-(Cyclohexylmethoxy)-9H-purin-2-amine;2-aMino-6-purine;2-aMino-6-[(cyclohexylMethyl)oxy]purine;2-Amino-6-(cyclohexylmethoxy)purine;NU-2058;O6-(CYCLOHEXYLMETHYL)GUANINE;NU2058> | | CAS: | 161058-83-9 | | MF: | C12H17N5O | | MW: | 247.3 | | EINECS: | | | Product Categories: | Protein Kinase;Cell Cycle Regulation | | Mol File: | 161058-83-9.mol |  |
| | NU 2058 Chemical Properties |
| Melting point | 199°C(lit.) | | Boiling point | 424.8±55.0 °C(Predicted) | | density | 1.52±0.1 g/cm3(Predicted) | | storage temp. | Keep in dark place,Sealed in dry,2-8°C | | solubility | DMSO: 22 mg/mL | | pka | 7.36±0.20(Predicted) | | form | powder to crystal | | color | white | | λmax | 281nm(MeOH)(lit.) | | InChI | InChI=1S/C12H17N5O/c13-12-16-10-9(14-7-15-10)11(17-12)18-6-8-4-2-1-3-5-8/h7-8H,1-6H2,(H3,13,14,15,16,17) | | InChIKey | MWGXGTJJAOZBNW-UHFFFAOYSA-N | | SMILES | N1C2C(=NC(N)=NC=2OCC2CCCCC2)NC=1 |
| Hazard Codes | Xi | | Risk Statements | 36/37/38 | | Safety Statements | 26-36/37 | | WGK Germany | 3 | | HS Code | 2933.99.9000 |
| | NU 2058 Usage And Synthesis |
| Description | NU 2058 is an inhibitor of cyclin-dependent kinase 1 (Cdk1) and Cdk2 (IC50s = 7.0 and 17 μM, respectively). Increased Cdk activity is often associated with human tumors, and inhibitors of Cdks, including NU 2058, can arrest cell cycling in cancer cells in vitro. | | Uses | NU 2058 is an intermediate of NU 6140 (N925295), a cyclin-dependant kinase 2 inhibitor which demonstrates 10-36 fold selectivity against Cdk2-cyclin A. This selectivity induces cell-cycle arrest at the G2-M phase and potentiates the apoptotic effect of pacitaxel. | | Biological Activity | Cyclin-dependent kinase (cdk) 1 and cdk2 inhibitor (K i values are 5 and 12 μ M respectively). Inhibits growth of human tumor cells in vitro (mean GI 50 = 13 μ M). Also inhibits DNA topoisomerase II ATPase activity (IC 50 = 300 μ M). | | IC 50 | CDK1: 26 μM (IC50); CDK2: 17 μM (IC50); CDK2: 12 μM (Ki) | | storage | Store at +4°C | | References | [1] IAN R. HARDCASTLE. N2-Substituted O6-Cyclohexylmethylguanine Derivatives: Potent Inhibitors of Cyclin-Dependent Kinases 1 and 2[J]. Journal of Medicinal Chemistry, 2004, 47 15: 3710-3722. DOI: 10.1021/jm0311442
[2] ROGER J. GRIFFIN et al. et al. Structure-Based Design of 2 -Arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine Inhibitors of Cyclin-Dependent Kinases 1 and 2.[J]. ChemInform, 2003, 34 51. DOI: 10.1002/chin.200351143
[3] N JOHNSON. Pre-clinical evaluation of cyclin-dependent kinase 2 and 1 inhibition in anti-estrogen-sensitive and resistant breast cancer cells[J]. British Journal of Cancer, 2009, 102 2: 342-350. DOI: 10.1038/sj.bjc.6605479
[4] A C RIGAS N J C C N Robson. Therapeutic potential of CDK inhibitor NU2058 in androgen-independent prostate cancer[J]. Oncogene, 2007, 26 55: 7611-7619. DOI: 10.1038/sj.onc.1210586 |
| | NU 2058 Preparation Products And Raw materials |
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