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KU-0058948
- Soluble in 0.1N HCl(aq), DMSO and EtOH
- MF: C21H21FN4O2
- MW: 380.42
Description
Potent and specific PARP inhibitor (IC50: 3.4 nM for PARP1); KU-0058948 activates transfected extracellular signal-regulated kinase 8 (ERK8) in cells and induces cell cycle arrest and apoptosis of primary myeloid leukemic cells and myeloid leukemic cell lines in vitro. The hydrochloride salt form, KU-0058948 hydrochloride (Axon 2001) is also available.
More Information
| Parent CAS No. | 763111-49-5 |
|---|---|
| Chemical Name | 4-(3-(1,4-Diazepane-1-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one |
| MFCD | N.A. |
| Short Description | PARP1 inhibitor |
References
- H Farmer et al. Targeting the DNA repair defect in BRCA mutant cells as a therapeutic strategy. Nature 2005, 434, 917-921.
- K Ratnam and JA Low. Current Development of Clinical Inhibitors of Poly(ADP-Ribose) Polymerase in Oncology. Clin. Cancer Res. 2007, 13, 1383.
- NC Turner et al. A synthetic lethal siRNA screen identifying genes mediating sensitivity to a PARP inhibitor. EMBO J. 2008, 27, 1368-1377.
- T Hay et al. Poly(ADP-ribose) polymerase-1 inhibitor treatment regresses autochthonous Brca2/p53-mutant mammary tumors in vivo and delays tumor relapse in combination with carboplatin. Cancer Res. 2009, 69(9), 3850.
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