Rucaparib (free base) (Synonyms: AG014447) |
رقم الكتالوجGC13249
One-Click Copy Product Info
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Rucaparib (قاعدة حرة) (AG014699) هو مثبط فعال وفعال عن طريق الفم لبروتينات PARP (PARP-1 و PARP-2 و PARP-3) مع Ki من 1.4 نانومتر لـ PARP1. Rucaparib (القاعدة الحرة) هو مثبط متواضع لهكسوز 6 فوسفات ديهيدروجينيز (H6PD). يحتوي Rucaparib (القاعدة الحرة) على إمكانية إجراء أبحاث عن سرطان البروستاتا المقاوم للإخصاء (CRPC).
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Cas No.: 283173-50-2
Sample solution is provided at 25 µL, 10mM.
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.
| 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: | |
| Cas No. | 283173-50-2 | SDF | |
| المرادفات | AG014447 | ||
| Chemical Name | 8-fluoro-2-(4-((methylamino)methyl)phenyl)-4,5-dihydro-1H-azepino[5,4,3-cd]indol-6(3H)-one | ||
| Canonical SMILES | FC1=CC2=C3C(CCNC2=O)=C(C4=CC=C(CNC)C=C4)NC3=C1 | ||
| Formula | C19H18FN3O | M.Wt | 323.36 |
| الذوبان | ≥ 16.15mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0925 mL | 15.4626 mL | 30.9253 mL |
| 5 mM | 618.5 μL | 3.0925 mL | 6.1851 mL |
| 10 mM | 309.3 μL | 1.5463 mL | 3.0925 mL |
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Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)