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

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

Cat. No.: HY-10617B
Handling Instructions Technical Support

Rucaparib (AG014699) hydrochloride 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 hydrochloride is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib hydrochloride has the potential for castration-resistant prostate cancer (CRPC) research.

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

CAS No. : 773059-19-1

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of Rucaparib hydrochloride:

Other Forms of Rucaparib hydrochloride:

Rucaparib hydrochloride Related Antibodies

Top Publications Citing Use of Products

37 Publications Citing Use of MCE Rucaparib hydrochloride

Cell Proliferation/Viability Assay
Flow Cytometry
In Vivo Efficacy Study

    Rucaparib hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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.

    View All PARP Isoform Specific Products:

    View All Isoforms
    PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target

    PARP-1

    1.4 nM (Ki)

    PARP-2

     

    PARP-3

     

    In Vitro

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

    Rucaparib (AG014699) hydrochloride and AG14584 significantly increase Temozolomide toxicity. Rucaparib (1 mg/kg) hydrochloride significantly increases Temozolomide-induced body weight loss. Rucaparib (0.1 mg/kg) hydrochloride results 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) hydrochloride 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) hydrochloride has greatest antitumor effect with three complete regressions[2].
    Rucaparib (1 mg/kg; i.p.; daily for 5d) hydrochloride 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.

    Animal Model: Female athymic nude mice, implanted SW620 colorectal tumor cells (1 × 107 cells per animal) s.c.[1]
    Dosage: 0.1 mg/kg in combination with Temozolomide (p.o., 200 mg/kg), 0.05, 0.15, and 0.5 mg/kg in combination with Temozolomide (p.o., 68 mg/kg) or 10 mg/kg
    Administration: IP, single dose for 0.1 mg/kg and 10 mg/kg, five daily doses for 0-0.5 mg/kg
    Result: Significantly increased Temozolomide toxicity, showed outstanding chemosensitization potency and caused enhancement of Temozolomide-induced tumor growth delay.
    Animal Model: CD-1 nude mice bearing established Capan-1 xenografts[2]
    Dosage: 10 mg/kg or 50, 100 and 150 mg/kg
    Administration: IP for 10 mg/kg; PO for 50, 100 and 150 mg/kg, single dose (Pharmacokinetics)
    Result: Parent drug was detectable in the plasma only at 30 min after 10 mg/kg i.p and up to 4 h for 50–150 mg/kg p.o.. Was still detectable in most mice receiving oral rucaparib at 3 days. Does not easily cross the plasma membrane.
    Animal Model: CD-1 nude mice bearing established Capan-1 xenografts[2]
    Dosage: 10 mg/kg i.p. daily for 5 days per week for 6 weeks, 50 or 150 mg/kg p.o. daily × five weekly × six, 150 mg/kg p.o. once per week for 6 weeks or three times per week for 6 weeks, or 150 mg/kg p.o. daily for five days every 3 weeks
    Administration: IP or PO
    Result: 10 mg/kg i.p. significantly inhibited the growth of the tumor, daily oral administration at 150 mg/kg had an equivalent effect on tumor growth to 10 mg/kg i.p.. The schedule with the greatest antitumor effect was oral administration of 150 mg/kg on a once weekly schedule with three complete regressions.
    Animal Model: CD-1 nude mice, NB1691 and SHSY5Y xenografts[6]
    Dosage: 1 mg/kg
    Administration: IP, daily for 5 d in combination with Temozolomide (orally daily ×5 at a dose of 68 mg/kg)
    Result: Enhanced the antitumor activity of Temozolomide and indicated complete and sustained tumor regression.
    Molecular Weight

    359.83

    Formula

    C19H19ClFN3O
    CAS No.
    SMILES

    FC1=CC2=C3C(CCNC2=O)=C(C4=CC=C(CNC)C=C4)NC3=C1.[H]Cl
    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
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    Rucaparib hydrochloride Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2
    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:

    Rucaparib773059-19-1AG014699PF-01367338AG 014699AG-014699PF01367338PF 01367338PARPpoly ADP ribose polymeraseorallyPARP-1PARP-2PARP-3hexose-6-phosphate dehydrogenaseH6PDcastration-resistant prostate cancerCRPCInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Requested Quantity *

    Applicant Name *

    		 

    Salutation

    Email Address *

    		 

    Phone Number *

    Department

    		 

    Organization Name *

    City

    State

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Rucaparib hydrochloride
    Cat. No.:
    HY-10617B
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    SAFETY DATA SHEET (SDS)

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.