2. Cell Cycle/DNA Damage Epigenetics
  3. PARP
  4. Rucaparib acetate

Rucaparib acetate  (Synonyms: AG014699 acetate; PF-01367338 acetate)

Cat. No.: HY-10617D
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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.

For research use only. We do not sell to patients.

CAS No. : 773059-23-7

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Rucaparib acetate Related Antibodies

Top Publications Citing Use of Products

37 Publications Citing Use of MCE Rucaparib acetate

Cell Proliferation/Viability Assay
Flow Cytometry
In Vivo Efficacy Study

    Rucaparib acetate 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 acetate 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).

    Rucaparib acetate purchased from MedChemExpress. Usage Cited in: Sci Adv. Sci Adv. 2025 Apr 25;11(17):eadu0847.

    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).

    Rucaparib acetate 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 acetate 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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    PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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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].

    IC50 & Target[1]

    PARP-1

    1.4 nM (Ki)

    PARP-2

     

    PARP-3

     

    In Vitro

    Rucaparib (AG014699) acetate is a possible N-demethylation metabolite of AG14644[1].
    Rucaparib (0.1, 1, 10, 100 μM; 24 hours) acetate 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 acetate is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib acetate 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 acetate 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 acetate Related Antibodies
    In Vivo

    Rucaparib (AG014699) acetate and AG14584 significantly increase Temozolomide toxicity. Rucaparib (1 mg/kg) acetate significantly increases Temozolomide-induced body weight loss. Rucaparib (0.1 mg/kg) acetate esults in a 50% increase in the temozolomide-induced tumor growth delay[1].
    Rucaparib (10 mg/kg for i.p. or 50, 150 mg/kg for p.o.; daily for 5 days per week for 6 weeks) acetate 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) acetate has greatest antitumor effect with three complete regressions[2].
    Rucaparib acetate 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.
    Molecular Weight

    383.42

    Formula

    C21H22FN3O3
    CAS No.
    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Purity & Documentation
    References
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    Rucaparib acetate Related Classifications

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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Rucaparib773059-23-7AG014699PF-01367338AG 014699AG-014699PF01367338PF 01367338PARPpoly ADP ribose polymeraseorallyPARP-1PARP-2PARP-3hexose-6-phosphate dehydrogenaseH6PDcastration-resistant prostate cancerCRPCInhibitorinhibitorinhibit

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