2,4-Pyrimidinediamine, 6-(cyclohexylmethoxy)-5-nitroso-
6-(cyclohexylmethoxy)-5-nitrosopyrimidine-2,4-diamine
CAS: 220036-08-8
Molecular Formula: C11H17N5O2
2,4-Pyrimidinediamine, 6-(cyclohexylmethoxy)-5-nitroso- - Names and Identifiers
| Name | 6-(cyclohexylmethoxy)-5-nitrosopyrimidine-2,4-diamine |
| Synonyms | NU6027 NU 6027 NU-6027 6-(cyclohexylmethoxy)-5-nitrosopyrimidine-2,4-diamine 2,6-DiaMino-4-(cyclohexylMethoxy)-5-nitrosopyriMidine 2,4-Pyrimidinediamine, 6-(cyclohexylmethoxy)-5-nitroso- |
| CAS | 220036-08-8 |
| InChI | InChI=1/C11H17N5O2/c12-9-8(16-17)10(15-11(13)14-9)18-6-7-4-2-1-3-5-7/h7H,1-6H2,(H4,12,13,14,15) |
2,4-Pyrimidinediamine, 6-(cyclohexylmethoxy)-5-nitroso- - Physico-chemical Properties
| Molecular Formula | C11H17N5O2 |
| Molar Mass | 251.29 |
| Density | 1.53±0.1 g/cm3(Predicted) |
| Melting Point | 252.5-253.7°C(lit.) |
| Boling Point | 549.2±60.0 °C(Predicted) |
| Flash Point | 286°C |
| Solubility | DMSO: 15mg/mL |
| Vapor Presure | 4.1E-12mmHg at 25°C |
| Appearance | Reddish-purple powder |
| Color | lavender |
| pKa | 2.52±0.10(Predicted) |
| Storage Condition | 2-8°C |
| Refractive Index | 1.698 |
| MDL | MFCD05664735 |
| Use | A selective inhibitor of cyclin-dependent kinase-2 (CDK2). |
| In vitro study | NU6027(100 μm) inhibited human tumor cell growth with an average GI50 of 10 μm. NU6027 acted on MCF7 cells, resulting in a decrease in the number of cells in S phase, while having no effect on G1 or G2/M phase. NU6027 is an effective inhibitor of intracellular ATR activity, acting on MCF7 cells with IC50 of 6.7 μm and GM847KD cells with IC50 of 2.8 μm, and enhancing the cytotoxicity of Hydroxyurea and Cisplatin, this effect is ATR-dependent. NU6027(10 μm) inhibited cdk2-regulated pRbT821 and pCHK1S345 by 42% and 70%, respectively. NU6027 acted on MCF7 cells and significantly enhanced Cisplatin (1.4-fold at 4 μm and 8.7-fold at 10 μm), Doxorubicin (1.3-fold at 4 μm, 2.5 times at 10 μm), Camptothecin (1.4 times at 4 μm, 2 times at 10 μm), and Hydroxyurea (1.8 times at 4 μm). NU6027 also enhanced 2GY IR in a concentration-dependent manner, and also enhanced the cytotoxicity of Camptothecin and Temozolomide (DNA methylating agent). Treatment of EM-C11 cells with NU6027(4 μm) enhanced early apoptosis to 7.5 percent after 48 hours, compared to 1.73 percent in untreated control cells. NU6027(10 μm) treatment of xrcc1-deficient OVCAR-4 cells decreased survival. NU6027 acts on XRCC1 deficient OVCAR-3 cells to enhance the cytotoxicity of Cisplatin. NU6027 acts on xrcc1-deficient OVCAR-3 cells to enhance Cisplatin-induced DSB accumulation. |
2,4-Pyrimidinediamine, 6-(cyclohexylmethoxy)-5-nitroso- - Risk and Safety
| WGK Germany | 3 |
2,4-Pyrimidinediamine, 6-(cyclohexylmethoxy)-5-nitroso- - Introduction
NU6027 is a potent ATR/CDK inhibitor. When CDK1/2, ATR and DNA-PK are inhibited, the Ki is 2.5 μM/1.3 μM, 0.4 μM and 2.2 μM, respectively, and it is easier to enter the cell than 6-aminopurine inhibitors.
Last Update：2022-10-16 17:15:01
2,4-Pyrimidinediamine, 6-(cyclohexylmethoxy)-5-nitroso- - Reference Information
| biological activity | NU6027 is an effective ATR/CDK inhibitor. when inhibiting CDK1/2, ATR and DNA-PK, Ki is 2.5 μM/1.3 μM, 0.4 μM and 2.2 μM respectively, which is easier to enter cells than 6-aminopurine inhibitors. NU6027 is an effective ATR/CDK inhibitor. when inhibiting CDK1/2, ATR and DNA-PK, Ki is 2.5 μM/1.3 μM, 0.4 μM and 2.2 μM respectively. it is easier to enter cells than 6-aminopurine inhibitors. |
| features | NU6027 inhibits cdk1 and cdk2 better than NU2058. |
| Target | Value |
| ATR | 0.4 μM(Ki) |
| CDK2 | 1.3 μM(Ki) |
| DNA-PK | 2.2 μM(Ki) |
| CDK1 | 2.5 μM(Ki) |
Last Update：2024-04-10 22:29:15
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CAS: 220036-08-8
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Mobile: 18021002903
QQ: 3008007409
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CAS: 220036-08-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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