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Nu 6027

Catalog No.
A1986
ATR/CDK inhibitor, potent and selective
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$83.00
In stock
5mg
$76.00
In stock
10mg
$120.00
In stock
50mg
$472.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt251.28
Cas No.220036-08-8
FormulaC11H17N5O2
Solubilityinsoluble in H2O; ≥12.55 mg/mL in DMSO; ≥2.72 mg/mL in EtOH with gentle warming and ultrasonic
Chemical Name6-(cyclohexylmethoxy)-5-nitrosopyrimidine-2,4-diamine
SDFDownload SDF
Canonical SMILESC1CCC(CC1)COC2=NC(=NC(=C2N=O)N)N
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

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

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Chemical structure

Nu 6027