2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Biological activity
Description
Target:
CDK1:2.5 μM (Ki)
CDK2:1.3 μM (Ki)
ATR
In Vivo
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.
Kinase Assay
Cell Assay
Animal Administration
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.
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