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

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

Cat. No.: HY-102003 Purity: 99.91%
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Rucaparib (AG014699) monocamsylate est un inhibiteur de PARP avec un Ki de 1,4 nM pour PARP1. Rucaparib monocamsylate montre également une affinité de liaison avec 8 autres domaines PARP.

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

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

CAS No. : 1859053-21-6

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Customer Review

Based on 39 publication(s) in Google Scholar

Other Forms of Rucaparib monocamsylate:

Rucaparib monocamsylate Related Antibodies

Top Publications Citing Use of Products

39 Publications Citing Use of MCE Rucaparib monocamsylate

Cell Proliferation/Viability Assay
Flow Cytometry
In Vivo Efficacy Study

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

    IC50 & Target[1][4]

    PARP-1

    1.4 nM (Ki)

    PARP-2

     

    PARP-3

     

    In Vitro

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

    Rucaparib (AG014699) monocamsylate and AG14584 significantly increase Temozolomide toxicity. Rucaparib (1 mg/kg) monocamsylate significantly increases Temozolomide-induced body weight loss. Rucaparib (0.1 mg/kg) monocamsylate 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) monocamsylate 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) monocamsylate has greatest antitumor effect with three complete regressions[2].
    Rucaparib monocamsylate 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 CD-1 nude mice aged 10-12 weeks with Capan-1 cells[2]
    Dosage: 10 mg/kg or 50, 150 mg/kg
    Administration: 10 mg/kg for i.p. or 50, 150 mg/kg for p.o.
    Result: Significantly inhibited the growth of the tumor.
    Molecular Weight

    555.66

    Formula

    C29H34FN3O5S
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to gray

    SMILES

    FC1=CC2=C3C(CCNC2=O)=C(C4=CC=C(CNC)C=C4)NC3=C1.O=S(C[C@@]5(C6(C)C)C(C[C@@]6([H])CC5)=O)(O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (89.98 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7997 mL 8.9983 mL 17.9966 mL
    5 mM 0.3599 mL 1.7997 mL 3.5993 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (3.74 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (3.74 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.91%

    SDS (418 KB)

    COA (254 KB) HNMR (186 KB) LCMS (98 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7997 mL 8.9983 mL 17.9966 mL 44.9915 mL
    5 mM 0.3599 mL 1.7997 mL 3.5993 mL 8.9983 mL
    10 mM 0.1800 mL 0.8998 mL 1.7997 mL 4.4992 mL
    15 mM 0.1200 mL 0.5999 mL 1.1998 mL 2.9994 mL
    20 mM 0.0900 mL 0.4499 mL 0.8998 mL 2.2496 mL
    25 mM 0.0720 mL 0.3599 mL 0.7199 mL 1.7997 mL
    30 mM 0.0600 mL 0.2999 mL 0.5999 mL 1.4997 mL
    40 mM 0.0450 mL 0.2250 mL 0.4499 mL 1.1248 mL
    50 mM 0.0360 mL 0.1800 mL 0.3599 mL 0.8998 mL
    60 mM 0.0300 mL 0.1500 mL 0.2999 mL 0.7499 mL
    80 mM 0.0225 mL 0.1125 mL 0.2250 mL 0.5624 mL
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    Rucaparib monocamsylate Related Classifications

    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:

    Rucaparib monocamsylate1859053-21-6AG014699 monocamsylate PF-01367338 monocamsylatePARPpoly ADP ribose polymeraseAG14644Capan-1BRCA2MX-1BRCA1NF-κBSSBrepairH6PDInhibitorinhibitorinhibit

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