189299

ATR/CDK Inhibitor, NU6027

The ATR/CDK Inhibitor, NU6027, also referenced under CAS 220036-08-8, controls the biological activity of ATR/CDK. This small molecule/inhibitor is primarily used for Cancer applications.

• Synonyma: ATR/CDK Inhibitor, NU6027, ATR Inhibitor, NU6027, 2,6-diamino-4-cyclohexyl-methyloxy-5-nitroso-pyrimidine, CDK2 Inhibitor, NU6027
• Empirický vzorec (Hillův zápis): C₁₁H₁₇N₅O₂
• Číslo CAS: 220036-08-8
• Molekulová hmotnost: 251.28
• MDL number: MFCD05664735
• UNSPSC Code: 12352200
• NACRES: NA.77

Vlastnosti

• Quality Level: 100
• assay: ≥98% (HPLC)
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: red-purple
• solubility: DMSO: 10 mg/mL, clear, blue
• shipped in: ambient
• storage temp.: −20°C
• SMILES string: Nc1nc(c(c(n1)OCC2CCCCC2)N=O)N
• InChI: 1S/C11H17N5O2/c12-9-8(16-17)10(15-11(13)14-9)18-6-7-4-2-1-3-5-7/h7H,1-6H2,(H4,12,13,14,15)
• InChI key: DGWXOLHKVGDQLN-UHFFFAOYSA-N

Popis

General description

A cell-permeable, pyrimidine derivative that acts as an ATP-competitive CDK Inhibitor (K_i = 2.5 µM for CDK1, and K_i = 1.3 µM for CDK2), and demonstrates cytostatic properties among a panel of 57 cancer cell lines. Also inhibits ATR kinase (IC₅₀ = 6.7 µM 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 10 µM, 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.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

Peasland, A., et al. 2011., Br J Cancer. 105, 372.
Arris, C.E, et al. 2000., J Med Chem.43, 2797.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Bezpečnostní informace

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable