Rucaparib tartrate
Based on 38 publication(s) in Google Scholar
Rucaparib (AG014699) tartrate 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 tartrate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib tartrate has the potential for castration-resistant prostate cancer (CRPC) research.
For research use only. We do not sell to patients.
- CAS No.: 773059-22-6
- Formula: C23H24FN3O7
- Molecular Weight:473.45
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Rucaparib tartrate
More- Nat Methods. 2023 Sep;20(9):1388-1399. [Abstract]
- Sci Immunol. 2024 Mar 15;9(93):eadj7238. [Abstract]
- Nat Commun. 2025 Jun 2;16(1):5126. [Abstract]
- Sci Transl Med. 2021 May 26;13(595):eabe8226. [Abstract]
- J Clin Invest. 2026 Mar 17:e200260. [Abstract]
- Theranostics. 2020 Jul 25;10(21):9477-9494. [Abstract]
- Sci Adv. Sci Adv. 2025 Apr 25;11(17):eadu0847. [Abstract]
- Sci Adv. 2022 Feb 18;8(7):eabl9794. [Abstract]
- Clin Cancer Res. 2017 Feb 15;23(4):1001-1011. [Abstract]
- Genes Dis. 2023 Apr 12;11(2):993-1008. [Abstract]
- Neoplasia. 2025 May:63:101152. [Abstract]
- Eur J Nucl Med Mol Imaging. 2024 Nov;51(13):4099-4110. [Abstract]
- JCI Insight. 2023 Nov 8;8(21):e165268. [Abstract]
- Talanta. 2018 Apr 1:180:127-132. [Abstract]
- Mol Cancer Ther. 2025 Jul 2. [Abstract]
- Mol Cancer Ther. 2024 Oct 1;23(10):1404-1417. [Abstract]
- Int J Mol Sci. 2020 Feb 11;21(4):1185. [Abstract]
- Cancers (Basel). 2024 Nov 5;16(22):3728. [Abstract]
- FASEB J. 2022 Jul;36(7):e22418. [Abstract]
- Neurooncol Adv. 2023 Feb 10;5(1):vdad010. [Abstract]
- Aging (Albany NY). 2021 Jan 20;13(3):4242-4257. [Abstract]
- BMC Cancer. 2022 Mar 23;22(1):312. [Abstract]
- Front Oncol. 2021 Jul 9:11:681441. [Abstract]
- Am J Cancer Res. 2024 Jan 15;14(1):378-389. [Abstract]
- Am J Cancer Res. 2020 Aug 1;10(8):2649-2676. [Abstract]
- DNA Repair. 2019 Jan:73:64-70. [Abstract]
- Gene. 2020 Oct 30;759:145000. [Abstract]
- Res Sq. 2026 Jun 17.
- bioRxiv. 2026 Mar 18.
- Research Square Preprint. 2024 Nov 06.
- bioRxiv. 2024 Sep 19:2024.09.19.613696. [Abstract]
- bioRxiv. 2024 Jul 10:2024.07.09.602803. [Abstract]
- bioRxiv. 2023 Feb 6:2023.02.06.527366. [Abstract]
- bioRxiv. 2023 Feb 7:2023.02.07.527369. [Abstract]
- Research Square Print. September 20th, 2022.
- Research Square Print. September 22nd, 2022.
- Patent. US20180362972A1.
- Patent. US20180263995A1.
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Cell Proliferation/Viability Assay
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Flow Cytometry
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
Biological Activity
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PARP-1 1.4 nM (Ki) |
PARP-2 |
PARP-3 |
Rucaparib (AG014699) tartrate is a possible N-demethylation metabolite of AG14644[1].
Rucaparib (0.1, 1, 10, 100 μM; 24 hours) tartrate is cytotoxic and has the LC50 being 5 μM in Capan-1 (BRCA2 mutant) cells and only 100 nM in MX-1 (BRCA1 mutant) cells[2].
The radio-sensitization by Rucaparib tartrate is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib tartrate can target NF-κB activated by DNA damage and overcome toxicity observed with classical NF-κB inhibitors without compromising other vital inflammatory functions[5].
Rucaparib tartrate inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilised D283Med cells[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rucaparib (10 mg/kg for i.p. or 50, 150 mg/kg for p.o.; daily for 5 days per week for 6 weeks) tartrate significantly inhibits the growth of the tumor, and there is one complete tumor regression and two persistent partial regressions[2].
Rucaparib (150 mg/kg; p.o.; once per week for 6 weeks or three times per week for 6 weeks) tartrate has greatest antitumor effect with three complete regressions[2].
Rucaparib tartrate enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 773059-22-6
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Molecular Weight 473.45
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Formula C23H24FN3O7
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SMILES
FC1=CC2=C3C(CCNC2=O)=C(C4=CC=C(CNC)C=C4)NC3=C1.OC([C@H](O)[C@@H](O)C(O)=O)=O
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Synonyms
AG-014699 tartrate; PF-01367338 tartrate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (38)
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Journal Impact Factor
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Most Recent
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Nat Methods
2023 Sep;20(9):1388-1399. PMID: 37474806 -
Sci Immunol
2024 Mar 15;9(93):eadj7238. PMID: 38489349 -
Nat Commun
Selective targeting of genome amplifications and repeat elements by CRISPR-Cas9 nickases to promote cancer cell death. [Abstract]2025 Jun 2;16(1):5126. PMID: 40456709
Rucaparib tartrate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jun 2;16(1):5126. [Abstract]
Treatment of MYCN-amplified SK-N-BE(2)C, KELLY, NGP, and CHP-212 or MYCN non-amplified SH-SY5Y neuroblastoma cells expressing) LINE-1 or MYCN targeting sgRNA with Cas9D10A-mRNA (7.5, 15, or 30 nM; increase in concentration marked by black triangle) without or with the PARP inhibitor, Rucaparib (10 µM). Inhibition of PARP1 in the presence of Cas9D10A is protective, as indicated in the reduced cell-killing efficacy of Cas9D10A at 3-days post-treatment (n = 3). PARP1 inhibition only had a modest effect on cell killing in KELLY and CHP-212 cells. A modest reduction in cell viability in SH-SY5Y cells in the presence of the PARP inhibitor is likely due to non-specific toxicity. Data are presented as mean ± s.d. normalized relative to viability of cells expressing AAVS1 targeting sgRNA treated with Cas9D10A.
Rucaparib tartrate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jun 2;16(1):5126. [Abstract]
Representative histograms of flow cytometric cell cycle analysis of SK-N-BE(2)C cells supplemented with PARP inhibitors at their respective IC50. SK-N-BE(2)C cells were incubated with Rucaparib (10 µM) or Olaparib (10 µM) in the absence of Cas9D10A and monitored for abberations in cell cycle progression at 1-, 2-, and 3-days (n = 3).
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Sci Transl Med
Hexose-6-phosphate dehydrogenase blockade reverses prostate cancer drug resistance in xenograft models by glucocorticoid inactivation. [Abstract]2021 May 26;13(595):eabe8226. PMID: 34039740
Rucaparib tartrate purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2021 May 26;13(595):eabe8226. [Abstract]
Viability of enz-resistant LAPC4 cells treated with Rucaparib (RUCA, 10-40 μM). Cells were treated with 100 nM cortisol with 10 μM Enzalutamide (enz) combined with the indicated drugs for 5 days and assayed using CellTiter-Glo. Viability is normalized to Ctrl.
Rucaparib tartrate purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2021 May 26;13(595):eabe8226. [Abstract]
Rucaparib (RUCA, 150 mg/kg; oral gavage BID, 5 days on, 2 days off) and the inhibitory effect of Enzalutamide (Enz) on xenograft growth in the F, VCaP and H, LAPC4 mouse xenograft models.
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J Clin Invest
Targeting Wnt/β-Catenin and circadian regulator restores PRC2/EZH2 controlled chromatin bivalency and suppresses cell state diversity. [Abstract]2026 Mar 17:e200260. PMID: 41842971 -
Theranostics
Molecular signatures of BRCAness analysis identifies PARP inhibitor Niraparib as a novel targeted therapeutic strategy for soft tissue Sarcomas. [Abstract]2020 Jul 25;10(21):9477-9494. PMID: 32863940 -
Sci Adv
Acute BRCAness induction and AR pathway blockage through CDK12/7/9 degradation enhances PARP inhibitor sensitivity in prostate cancer. [Abstract]Sci Adv. 2025 Apr 25;11(17):eadu0847. PMID: 40267193
Rucaparib tartrate purchased from MedChemExpress. Usage Cited in: Sci Adv. Sci Adv. 2025 Apr 25;11(17):eadu0847. [Abstract]
Cell viability assays in LNCaP and 22Rv1 cells treated with BSJ-5-63 for 2 days, PARPis [olaparib (Ola), Rucaparib (Ruca; 3 μM), niraparib (Nira), or talazoparib (Tala)] for 7 days, or sequential combination where BSJ-5-63 was removed after 2 days and followed by PARPi treatment for additional 5 days. Data represent means ± SEM (n = 3).
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Sci Adv
RB1 loss overrides PARP inhibitor sensitivity driven by RNASEH2B loss in prostate cancer. [Abstract]2022 Feb 18;8(7):eabl9794. PMID: 35179959 -
Clin Cancer Res
Drug-Driven Synthetic Lethality: Bypassing Tumor Cell Genetics with a Combination of AsiDNA and PARP Inhibitors. [Abstract]2017 Feb 15;23(4):1001-1011. PMID: 27559053 -
Genes Dis
The m6A regulator KIAA1429 stabilizes RAB27B mRNA and promotes the progression of chronic myeloid leukemia and resistance to targeted therapy. [Abstract]2023 Apr 12;11(2):993-1008. PMID: 37692484 -
Neoplasia
Targeting BARD1 suppresses a Myc-dependent transcriptional program and tumor growth in pancreatic ductal adenocarcinoma. [Abstract]2025 May:63:101152. PMID: 40096771 -
Eur J Nucl Med Mol Imaging
Combining [177Lu]Lu-DOTA-TOC PRRT with PARP inhibitors to enhance treatment efficacy in small cell lung cancer. [Abstract]2024 Nov;51(13):4099-4110. PMID: 39023784 -
JCI Insight
Mutant RB1 enhances therapeutic efficacy of PARPis in lung adenocarcinoma by triggering the cGAS/STING pathway. [Abstract]2023 Nov 8;8(21):e165268. PMID: 37937640 -
Talanta
Ultrasensitive electrochemical detection of poly (ADP-ribose) polymerase-1 via polyaniline deposition. [Abstract]2018 Apr 1:180:127-132. PMID: 29332790 -
Mol Cancer Ther
Harnessing senolytics and PARP inhibition to expand the antitumor activity of CDK4/6 inhibitors in prostate cancer. [Abstract]2025 Jul 2. PMID: 40601842 -
Mol Cancer Ther
AKT Inhibition Sensitizes to Polo-Like Kinase 1 Inhibitor Onvansertib in Prostate Cancer. [Abstract]2024 Oct 1;23(10):1404-1417. PMID: 38894678 -
Int J Mol Sci
2020 Feb 11;21(4):1185. PMID: 32053991 -
Cancers (Basel)
2024 Nov 5;16(22):3728. PMID: 39594684 -
FASEB J
LPS stimulation stabilizes HIF-1α by enhancing HIF-1α acetylation via the PARP1-SIRT1 and ACLY-Tip60 pathways in macrophages. [Abstract]2022 Jul;36(7):e22418. PMID: 35713568 -
Neurooncol Adv
The PARP inhibitor Rucaparib synergizes with radiation to attenuate atypical teratoid rhabdoid tumor growth. [Abstract]2023 Feb 10;5(1):vdad010. PMID: 36915612 -
Aging (Albany NY)
Oxaliplatin induces the PARP1-mediated parthanatos in oral squamous cell carcinoma by increasing production of ROS. [Abstract]2021 Jan 20;13(3):4242-4257. PMID: 33495407 -
BMC Cancer
PARP inhibitors chemopotentiate and synergize with cisplatin to inhibit bladder cancer cell survival and tumor growth. [Abstract]2022 Mar 23;22(1):312. PMID: 35321693 -
Front Oncol
The Emerging Role of Poly (ADP-Ribose) Polymerase Inhibitors as Effective Therapeutic Agents in Renal Cell Carcinoma. [Abstract]2021 Jul 9:11:681441. PMID: 34307148 -
Am J Cancer Res
Novel dual action PARP and microtubule polymerization inhibitor AMXI-5001 powerfully inhibits growth of esophageal carcinoma both alone and in combination with radiotherapy. [Abstract]2024 Jan 15;14(1):378-389. PMID: 38323288 -
Am J Cancer Res
AMXI-5001, a novel dual parp1/2 and microtubule polymerization inhibitor for the treatment of human cancers. [Abstract]2020 Aug 1;10(8):2649-2676. PMID: 32905466 -
DNA Repair
Loss of the p12 subunit of DNA polymerase delta leads to a defect in HR and sensitization to PARP inhibitors. [Abstract]2019 Jan:73:64-70. PMID: 30470508 -
Gene
Rucaparib antagonize multidrug resistance in cervical cancer cells through blocking the function of ABC transporters. [Abstract]2020 Oct 30;759:145000. PMID: 32717310 -
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bioRxiv
2024 Sep 19:2024.09.19.613696. PMID: 39345583 -
bioRxiv
Acute BRCAness Induction and AR Signaling Blockage through CDK12/7/9 Degradation Enhances PARP Inhibitor Sensitivity in Prostate Cancer. [Abstract]2024 Jul 10:2024.07.09.602803. PMID: 39026842 -
bioRxiv
Mono-ADP-ribosyltransferase 1 ( Artc1 )-deficiency decreases tumorigenesis, increases inflammation, decreases cardiac contractility, and reduces survival. [Abstract]2023 Feb 6:2023.02.06.527366. PMID: 36945646 -
bioRxiv
A PARP inhibitor, rucaparib, improves cardiac dysfunction in ADP-ribose-acceptor hydrolase 3 ( Arh3 ) deficiency. [Abstract]2023 Feb 7:2023.02.07.527369. PMID: 36945462 -
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Purity & Documentation
References
[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. [Content Brief]
[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. [Content Brief]
[3]. Matt Shirley, et al. Rucaparib: A Review in Ovarian Cancer. Target Oncol. 2019 Apr;14(2):237-246. [Content Brief]
[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. [Content Brief]
[5]. Hunter JE, et al. NF-κB mediates radio-sensitization by the PARP-1 inhibitor, AG-014699. Oncogene, 2012, 31(2), 251-264. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)