Cas No.: | 220036-08-8 |
Chemical Name: | 4-Cyclohexylmethoxy-2,6-diamino-5-nitrosopyrimidine |
Synonyms: | NU6027,NU-6027,NU 6027 |
SMILES: | NC1=NC(OCC2CCCCC2)=C(N=O)C(N)=N1 |
Formula: | C11H17N5O2 |
M.Wt: | 251.28 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | NU6027 is a potent and ATP-competitive inhibitor of both CDK1 and CDK2, with Kis of 2.5 μM and 1.3 μM, respectively. NU6027 is also a potent inhibitor of ATR and enhances hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner[1][2]. |
Target: | CDK1:2.5 μM (Ki) CDK2:1.3 μM (Ki) ATR |
In Vitro: | NU6027 (1 nM-100 μM; 48 h) inhibits the growth of human tumor cells with a GI50 of 10±6 μM[1]. NU6027 (0.1-25 μM; 24 h) inhibits ATR activity with an IC50 of 2.8 μM in GM847KD cells. NU6027 (1-10 μM; 24 h) inhibits ATR activity with an IC50 of 6.7±2.3 μM in MCF7 cells[2]. NU6027 (4 or 10 μM; 24 h) attenuates G2/M arrest following DNA damage in MCF7 cells[2]. NU6027 (10 μM; 24 h) significantly reduces RAD51 foci in both control and PF-01367338-treated V-C8 B2 cells[2]. NU6027 (4 μM; 24 h) causes 82% suppression of the increase in RAD51 foci-positive cells treated by PF-01367338[2]. Western Blot Analysis[2] Cell Line: MCF7 cells Concentration: 0, 1, 5, 10 μM Incubation Time: 24 h Result: Inhibited CDK2-mediated pRbT821 by 42±27% compared with 70±12% inhibition of pCHK1S345 with the concentration of 10 μM. |
References: | [1]. Arris CE, et, al. Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles. J Med Chem. 2000 Jul 27; 43(15): 2797-804. [2]. Peasland A, et, al. Identification and evaluation of a potent novel ATR inhibitor, NU6027, in breast and ovarian cancer cell lines. Br J Cancer. 2011 Jul 26;105(3):372-81. |