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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

CAS Number

[283173-50-2]

Product Name Alternative

AG014699; PF-01367338

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

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.html

Concentration

10mM

Purity

99.97

Solubility

DMSO : 70 mg/mL (ultrasonic; warming; heat to 60°C) |H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

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

Molecular Formula

C19H18FN3O

Molecular Weight

323.36

Precautions

H302, H315, H319, H335

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]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.|[6]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.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Launched

Isoform

PARP1; PARP2; PARP3

Citation 01

Aging (Albany NY) . 2021 Jan 20;13 (3) :4242-4257.|Am J Cancer Res. 2020 Aug 1;10 (8) :2649-2676.|Am J Cancer Res. 2024 Jan 15;14 (1) :378-389.|bioRxiv. 2023 Feb 6:2023.02.06.527366.|bioRxiv. 2023 Feb 7:2023.02.07.527369.|bioRxiv. 2024 Jul 10:2024.07.09.602803.|bioRxiv. 2024 Sep 19:2024.09.19.613696.|BMC Cancer. 2022 Mar 23;22 (1) :312.|Cancers (Basel) . 2024 Nov 5;16 (22) :3728.|Clin Cancer Res. 2017 Feb 15;23 (4) :1001-1011. |DNA Repair. 2019 Jan:73:64-70.|Eur J Nucl Med Mol Imaging. 2024 Nov;51 (13) :4099-4110.|FASEB J. 2022 Jul;36 (7) :e22418.|Front Oncol. 2021 Jul 9:11:681441.|Gene. 2020 Oct 30;759:145000.|Genes Dis. 2023 Apr 12;11 (2) :993-1008.|Int J Mol Sci. 2020 Feb 11;21 (4) :1185.|JCI Insight. 2023 Nov 8;8 (21) :e165268.|Mol Cancer Ther. 2024 Oct 1;23 (10) :1404-1417.|Mol Cancer Ther. 2025 Jul 2.|Nat Commun. 2025 Jun 2;16 (1) :5126.|Nat Methods. 2023 Sep;20 (9) :1388-1399.|Neoplasia. 2025 May:63:101152.|Neurooncol Adv. 2023 Feb 10;5 (1) :vdad010.|Patent. US20180263995A1.|Patent. US20180362972A1.|Research Square Preprint. 2024 Nov 06.|Research Square Print. September 20th, 2022.|Research Square Print. September 22nd, 2022.|Sci Adv. 2022 Feb 18;8 (7) :eabl9794.|Sci Adv. Sci Adv. 2025 Apr 25;11 (17) :eadu0847.|Sci Immunol. 2024 Mar 15;9 (93) :eadj7238.|Sci Transl Med. 2021 May 26;13 (595) :eabe8226.|Talanta. 2018 Apr 1:180:127-132.|Theranostics. 2020 Jul 25;10 (21) :9477-9494. |Analyst. 2018 May 29;143 (11) :2501-2507.|Biochem Biophys Res Commun. 28 September 2021.|J Mol Med (Berl) . 2019 Aug;97 (8) :1183-1193.|Nat Cell Biol. 2024 Sep;26 (9) :1545-1557.|Patent. US20200078369A1|Patent. US20200129476A1|PLoS One. 2024 Nov 1;19 (11) :e0308647.|Sens Actuators B Chem. 2018 Nov 10; 273:1047-1053. |Sens Actuators B Chem. 2018, 259: 565-572.|J Med Chem. 2023 Mar 23;66 (6) :4106-4130.|J Mol Med (Berl) . 2019 Aug;97 (8) :1183-1193.

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