Rucaparib (acetate)

CAT: 0804-HY-10617DSize: 1 EachDry Ice: NoHazardous: No
CAT#:0804-HY-10617DSize:1 Each
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Description
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].
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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
PARP1; PARP2; PARP3

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