Rucaparib (phosphate) (Standard)

Rucaparib (phosphate) (Standard) is the analytical standard of Rucaparib (phosphate) . This product is intended for research and analytical applications. Rucaparib (AG014699) phosphate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib phosphate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib phosphate has the potential for castration-resistant prostate cancer (CRPC) research[1][2][3][4].

Product Specifications

CAS Number

[459868-92-9]

Product Name Alternative

AG-014699 (phosphate) (Standard) ; PF-01367338 (phosphate) (Standard)

UNSPSC

12352005

Target

PARP; Reference Standards

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; Others

Field of Research

Cancer

Smiles

O=P(O)(O)O.FC1=CC2=C3C(CCNC2=O)=C(C4=CC=C(CNC)C=C4)NC3=C1

Molecular Formula

C19H21FN3O5P

Molecular Weight

421.36

References & Citations

[1]Thomas HD, et al. Preclinical selection of a novel poly (ADP-ribose) polymerase inhibitor for clinical trial. Mol Cancer Ther, 2007, 6 (3), 945-956.|[2]Hunter JE, et al. NF-κB mediates radio-sensitization by the PARP-1 inhibitor, AG-014699. Oncogene, 2012, 31 (2), 251-264.|[3]Daniel RA, et al. Inhibition of poly (ADP-ribose) polymerase-1 enhances temozolomide and topotecan activity against childhood neuroblastoma. Clin Cancer Res, 2009, 15 (4), 1241-1249.|[4]Matt Shirley, et al. Rucaparib: A Review in Ovarian Cancer. Target Oncol. 2019 Apr;14 (2) :237-246.|[5]Jianneng Li, et al. Hexose-6-phosphate dehydrogenase blockade reverses prostate cancer drug resistance in xenograft models by glucocorticoid inactivation. Sci Transl Med. 2021 May 26;13 (595) :eabe8226.|[6]J Murray, et al. Tumour cell retention of rucaparib, sustained PARP inhibition and efficacy of weekly as well as daily schedules. Br J Cancer. 2014 Apr 15;110 (8) :1977-84.