AG-014699/PF-01367338，AG-14447,AG014699

溶解度:Soluble in water

储存条件:-20C 2 years

生物活性

AG014699, the phosphate salt of AG14447, which has improved aqueous solubility, has been selected for clinical trial.AG014699 is a tricyclic indole poly(ADP-Ribose) polymerase (PARP) inhibitor with potential antineoplastic activity. PARP-1 inhibitor AG014699 blocks base excision repair mediated by PARP 1 on single strand breaks and may be particularly efficacious in inducing apoptosis in breast cancer associated gene-1 and -2 (BRCA1/2) deficient tumor cells.

参考文献

1. Plummer R, Jones C, Middleton M, Wilson R, Evans J, Olsen A, Curtin N, Boddy A, McHugh P, Newell D, Harris A, Johnson P, Steinfeldt H, Dewji R, Wang D, Robson L, Calvert H. Phase I study of the poly(ADP-ribose) polymerase inhibitor, AG014699, in combination with temozolomide in patients with advanced solid tumors. Clin Cancer Res. 2008 Dec 1;14(23):7917-23