Rucaparib (acetate)

Rucaparib (AG014699) acetate 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 acetate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib acetate has the potential for castration-resistant prostate cancer (CRPC) research[1][2][3][4].

Product Specifications

CAS Number

[773059-23-7]

Product Name Alternative

AG014699 (acetate) ; PF-01367338 (acetate)

UNSPSC

12352005

Target

PARP

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/rucaparib-acetate.html

Solubility

10 mM in DMSO

Smiles

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

Molecular Formula

C21H22FN3O3

Molecular Weight

383.42

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]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.|[3]Matt Shirley, et al. Rucaparib: A Review in Ovarian Cancer. Target Oncol. 2019 Apr;14 (2) :237-246.|[4]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.|[5]Hunter JE, et al. NF-κB mediates radio-sensitization by the PARP-1 inhibitor, AG-014699. Oncogene, 2012, 31 (2), 251-264.|[6]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.