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| Product | Description | |
|---|---|---|
| NU6027 | ?98% (HPLC). Group: Fluorescence/luminescence spectroscopy. |  |
| NU6027 | NU6027 is a potent inhibitor of cellular ATR activity (IC(50)=6.7 μM) and enhanced hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner. NU6027 attenuated G2/M arrest following DNA damage, inhibited RAD51 focus formation and increased the cytotoxicity of the major classes of DNA-damaging anticancer cytotoxic therapy but not the antimitotic, paclitaxel. In A2780 cells sensitisation to cisplatin was greatest in cells with functional p53 and mismatch repair (MMR) and sensitisation to temozolomide was greatest in p53 mutant cells with functional MMR. Importantly, NU6027 was synthetically lethal when DNA single-strand break repair is impaired either through poly(ADP-ribose) polymerase (PARP) inhibition or defects in XRCC1. NU6027 inhibits ATR, impairing G2/M arrest and homologous recombination thus increasing sensitivity to DNA-damaging agents and PARP inhibitors. It provides proof of concept data for clinical development of ATR inhibitors. Synonyms: NU-6027; NU 6027; 2,6-Diamino-4-(cyclohexylmethoxy)-5-nitrosopyrimidine; 6-(Cyclohexylmethoxy)-5-nitroso-2,4-pyrimidinediamine; 4-Cyclohexylmethoxy-2,6-diamino-5-nitrosopyrimidine; 4-Cyclohexylmethoxy-5-nitrosopyrimidine-2,6-diamine. Grades: ≥98%. CAS No. 220036-08-8. Molecular formula: C11H17N5O2. Mole weight: 251.29. |  |
| ATR/CDK Inhibitor, NU6027 (2,6-diamino-4-cyclohexyl-methyloxy-5-nitroso-pyrimidine, ATR Inhibitor, NU6027, CDK2 Inhibitor) | A cell-permeable, pyrimidine derivative that acts as an ATP-competitive CDK Inhibitor (Ki=2.5uM for CDK1, and Ki=1.3uM for CDK2), and demonstrates cytostatic properties among a panel of 57 cancer cell lines. Also inhibits ATR kinase (IC50=6.7uM in MCF7 cells), but does not interfere with irradiation-induced autophosphorylation of DNA-PK or ATM. Potentiates a range of DNA-damaging cytotoxic drugs such as hydroxyurea (1.8-fold) and cisplatin (1.4-fold) at 10uM, but not the anti-mitotic paclitaxel. Attenuates G2/M arrest following DNA damage and inhibits RAD51 focus formation. Shown to be synthetically lethal when DNA single-strand break repair is impaired in PARP-inhibited cells. Group: Biochemicals. Grades: Highly Purified. CAS No. 220036-08-8. Pack Sizes: 10mg. US Biological Life Sciences. |  Worldwide |
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