Rucaparib-d8

Rucaparib-d8 (AG014699-d8) is deuterium labeled Rucaparib. Rucaparib (AG014699) 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 is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib has the potential for castration-resistant prostate cancer (CRPC) research[1][2][3][4].

Product Specifications

Product Name Alternative

AG014699-d8 ; PF-01367338-d8

UNSPSC

12352005

Target

Isotope-Labeled Compounds; PARP

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; Others

Applications

Cancer-programmed cell death

Field of Research

Cancer

Smiles

O=C1NCCC2=C(C3=C([2H])C([2H])=C(C([2H])NC([2H])([2H])[2H])C([2H])=C3[2H])NC4=CC(F)=CC1=C42

Molecular Formula

C19H10D8FN3O

Molecular Weight

331.41

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]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.|[3]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.|[4]Hunter JE, et al. NF-κB mediates radio-sensitization by the PARP-1 inhibitor, AG-014699. Oncogene, 2012, 31 (2), 251-264.|[5]Matt Shirley, et al. Rucaparib: A Review in Ovarian Cancer. Target Oncol. 2019 Apr;14 (2) :237-246.|[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.|[7]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.