Toggle Nav
APExBIO

Nu 6027

In stock
Catalog No.
A1986
ATR/CDK inhibitor, potent and selective
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$70.00
In stock
5mg
$69.00
In stock
10mg
$109.00
In stock
50mg
$429.00
In stock

Tel: +1-832-696-8203

Email: sales@apexbt.com

Worldwide Distributors

NU6027 is a potent inhibitor of cellular ATR activity with the IC50 of 6.7 μM.
The ataxia telangiectasia mutated and Rad3-related kinase (ATR) has a crucial role in the stalled replication forks signalling and DNA damage to cell cycle checkpoints and DNA repair. ATR was recognised as an key target for cancer therapy, however, its inhibitors have proved elusive. NU6027, which was originally developed as a CDK2 inhibitor, inhibits ATR.
In vitro: NU6027 is a potent inhibitor of cellular ATR activity with the IC50 of 6.7 μM and enhanced the cytotoxicity of hydroxyurea and cisplatin in an ATR-dependent manner. NU6027 attenuated G2/M phase arrest with DNA damage, inhibited the formation of RAD51 focus and increased the cytotoxicity of the major classes of DNA-damaging cytotoxic therapy but not paclitaxel and antimitotic. In A2780 cells, cisplatin sensitisation was greatest in cells with functional p53 and mismatch repair and sensitisation to temozolomide was greatest in p53 mutant cells with functional mismatch repair. More importantly, NU6027 was found to be synthetically lethal when DNA single-strand break repair is impaired either through poly(ADP-ribose) polymerase (PARP) inhibition or defects in XRCC1 [1].
In vivo: Currently no in-vivo data are available.
Clinical trial: NU6027 is still in preclinical development stage and no clinicl trial is ongoing currently.
Reference:
[1] Peasland A, Wang LZ, Rowling E, Kyle S, Chen T, Hopkins A, Cliby WA, Sarkaria J, Beale G, Edmondson RJ, Curtin NJ. Identification and evaluation of a potent novel ATR inhibitor, NU6027, in breast and ovarian cancer cell lines. Br J Cancer. 2011;105(3):372-81.

Physical Appearance

A solid

Chemical Properties

StorageStore at -20°C
M.Wt251.28
Cas No.220036-08-8
FormulaC11H17N5O2
Solubility≥12.55mg/mL in DMSO
Chemical Name6-(cyclohexylmethoxy)-5-nitrosopyrimidine-2,4-diamine
SDFDownload SDF
Canonical SMILESC1CCC(CC1)COC2=NC(=NC(=C2N=O)N)N
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description Nu 6027 is a selective inhibitor of CDK1 and CDK2 with IC50 value of 2.9 and 2.2 µM, respectively.
Targets CDK1 CDK2        
IC50 2.9 µM 2.2 µM        

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

Nu 6027