General description
A cell-permeable, pyrimidine derivative that acts as an ATP-competitive CDK Inhibitor (Ki = 2.5 µM for CDK1, and Ki = 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
- UPC:
- 12352200
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 189299-10MG
