Rucaparib (free base)
Catalog No.: GC13249Purity:>99.00%Synonyms: AG014447
Rucaparib (free base) (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 (free base) is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib (free base) has the potential for castration-resistant prostate cancer (CRPC) research.
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Cas No.: 283173-50-2
10mM (in 1mL DMSO)In Stock
$59.00
1
5mgIn Stock
$53.00
1
10mgIn Stock
$99.00
1
50mgIn Stock
$258.00
1
200mgIn Stock
$585.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $59.00 | In Stock | 1 | |
| 5mg | $53.00 | In Stock | 1 | |
| 10mg | $99.00 | In Stock | 1 | |
| 50mg | $258.00 | In Stock | 1 | |
| 200mg | $585.00 | In Stock | 1 |
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Citations
2 publicationsPublications from researchers using this productDescription
Rucaparib (free base) is an orally bioavailable tricyclic indole poly (ADP-ribose) polymerase (PARP) inhibitor. Rucaparib phosphate blocks PARP-mediated DNA repair by selectively binding to and inhibiting the activity of PARP1 (Ki=1.4nM), PARP2, and PARP3, leading to accumulation of DNA strand breaks, genomic instability, and apoptosis. Rucaparib phosphate can be used in research related to BRCA mutation-associated ovarian cancer, fallopian tube cancer, primary peritoneal cancer, and metastatic castration-resistant prostate cancer (mCRPC)[1-4].
In vitro, Rucaparib phosphate (0.763nM-50μM) was used to treat CDK12 knockout (KO) prostate cancer cells (C42B, LNCaP) for 7 days. Rucaparib phosphate inhibited the growth of CDK12 KO cells[5]. Rucaparib phosphate (1.104-1.488μM) was combined with Trabectedin (0.352-2.64nM) to treat soft tissue sarcoma cell lines (IB115, IB111, IB136) for 72 hours. Rucaparib phosphate synergized with Trabectedin to inhibit cell proliferation, induce apoptosis, cause G2/M phase accumulation, and increase DNA damage[6].
In vivo, Rucaparib phosphate (150mg/kg) was orally administered to mice with lung adenocarcinoma (LP07) for 20 days. Rucaparib phosphate significantly reduced tumor burden, while decreasing PARP activity and cell proliferation, and increasing DNA damage, TUNEL-positive nuclei, protein oxidation, and SOD2 content[7]. Rucaparib phosphate (150mg/kg; five times per week) was orally administered to CD-1 nude mice bearing Capan-1 xenograft tumors for 6 weeks. Rucaparib phosphate significantly delayed tumor growth and induced tumor regression[8].
References:
[1] Fizazi K, Piulats JM, Reaume MN, et al. TRITON3 Investigators. Rucaparib or Physician's Choice in Metastatic Prostate Cancer. N Engl J Med. 2023 Feb 23;388(8):719-732.
[2] Thomas HD, Calabrese CR, Batey MA, et al. Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial. Mol Cancer Ther. 2007 Mar;6(3):945-56.
[3] Syed YY. Rucaparib: First Global Approval. Drugs. 2017 Apr;77(5):585-592.
[4] Shirley M. Rucaparib: A Review in Ovarian Cancer. Target Oncol. 2019 Apr;14(2):237-246.
[5] Chou J, Robinson TM, Egusa EA, et al. Synthetic Lethal Targeting of CDK12-Deficient Prostate Cancer with PARP Inhibitors. Clin Cancer Res. 2024 Dec 2;30(23):5445-5458.
[6] Laroche A, Chaire V, Le Loarer F, et al. Activity of trabectedin and the PARP inhibitor rucaparib in soft-tissue sarcomas. J Hematol Oncol. 2017 Apr 11;10(1):84.
[7] Pérez-Peiró M, Valentí-Serra P, León-González B, et al. Attenuation of Tumor Burden in Response to Rucaparib in Lung Adenocarcinoma: The Contribution of Oxidative Stress, Apoptosis, and DNA Damage. Int J Mol Sci. 2023 Jan 30;24(3):2580.
[8] Murray J, Thomas H, Berry P, 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.
Protocol
| Cell experiment [1]: | |
Cell lines | LNCaP, C42B, PC3, DLD-1, MDA-MB-231, CAOV3, OVCAR-8 (prostate cancer and other cancer cell lines) |
Preparation Method | Cells were maintained in RPMI-1640 or DMEM supplemented with 10% fetal bovine serum (FBS) under standard conditions. Cells were treated with Rucaparib phosphate or DMSO for seven days. |
Reaction Conditions | 0.763nM-50μM; 7 days |
Applications | Rucaparib phosphate preferentially inhibited the growth of CDK12 knockout (KO) cells compared to isogenic wild-type cells. CDK12 KO cells were more sensitive to Rucaparib phosphate than control cells. |
| Animal experiment [2]: | |
Animal models | BALB/c mice with LP07 lung adenocarcinoma tumors |
Preparation Method | Mice were subcutaneously injected with LP07 lung adenocarcinoma cells to generate tumors. Tumor-bearing mice were randomized into two groups: non-treated (control) and treated with Rucaparib phosphate (150mg/kg; p.o.). Treatment started when tumors became measurable. |
Dosage form | 150mg/kg; p.o.; 20 days |
Applications | Rucaparib phosphate treatment significantly reduced tumor weight and tumor area compared to non-treated controls. Rucaparib phosphate decreased PARP activity and cell proliferation, while increasing DNA damage, TUNEL-positive nuclei, protein oxidation, and superoxide dismutase 2 content within the tumors. |
References: | |
Product Documents
Purity:>99.00%Appearance:A solid
Chemical Properties
CAS No.
283173-50-2
Synonyms
AG014447
Chemical Name
8-fluoro-2-(4-((methylamino)methyl)phenyl)-4,5-dihydro-1H-azepino[5,4,3-cd]indol-6(3H)-one
SMILES
FC1=CC2=C3C(CCNC2=O)=C(C4=CC=C(CNC)C=C4)NC3=C1
Molecular Formula
C19H18FN3O
Molecular Weight
323.36
Solubility
≥ 16.15mg/mL in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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