Rucaparib (free base)Potent PARP inhibitor CAS# 283173-50-2 |
- MK-4827 hydrochloride
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- Rucaparib (AG-014699,PF-01367338)
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 283173-50-2 | SDF | Download SDF |
| PubChem ID | 9931954 | Appearance | Powder |
| Formula | C19H18FN3O | M.Wt | 323.36 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | AG014699; PF-01367338 | ||
| Solubility | >16.2mg/mL in DMSO | ||
| SMILES | CNCC1=CC=C(C=C1)C2=C3CCNC(=O)C4=CC(=CC(=C34)N2)F | ||
| Standard InChIKey | HMABYWSNWIZPAG-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C19H18FN3O/c1-21-10-11-2-4-12(5-3-11)18-14-6-7-22-19(24)15-8-13(20)9-16(23-18)17(14)15/h2-5,8-9,21,23H,6-7,10H2,1H3,(H,22,24) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP1 with Ki of 1.4 nM. | |||||
| Targets | PARP | |||||
| IC50 | 1.4 nM (Ki) | |||||
| Cell experiment [1]: | |
| Cell lines | Canine kidney MDCKII cell lines |
| Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
| Reacting condition | 8h; 5 μM |
| Applications | In the MDCKII parental cell line, which overexpressed human (h) ABCB1, both apically and basolaterally directed translocation of rucaparib were the same. Treatment of the cells with the ABCB1 inhibitor zosuquidar resulted in a slight decrease in apically directed transport, which could be either due to a specific inhibition of an unidentified rucaparib uptake transporter at the basolateral side, or inhibition of endogenous canine ABCB1. The result shown that rucaparib is a transported substrate of ABCB1. |
| Animal experiment [1]: | |
| Animal models | female WT, Abcb1a/1b mice of a >99% FVB genetic background |
| Dosage form | 10 mg/kg; oral taken |
| Application | We analyzed the separate and combined effect of Abcg2 and Abcb1a/1b activity on the in vivo disposition of orally administered rucaparib at a dose of 10 mg/kg in wild-type (WT) and single and combination Abcg2 and Abcb1a/1b knockout mice. In vivo, oral availability (plasma AUC0-1 and AUC0-24) and brain levels of rucaparib at 1 and 24 h were increased by the absence of both Abcg2 and Abcb1a/1b after oral administration of rucaparib at 10 mg/kg. |
| Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
| References: [1] Durmus S, Sparidans R W, van Esch A, et al. Breast Cancer Resistance Protein (BCRP/ABCG2) and P-glycoprotein (P-GP/ABCB1) Restrict Oral Availability and Brain Accumulation of the PARP Inhibitor Rucaparib (AG-014699)[J]. Pharmaceutical research, 2014: 1-10. | |
Rucaparib (free base) Dilution Calculator
Rucaparib (free base) Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.0925 mL | 15.4626 mL | 30.9253 mL | 61.8506 mL | 77.3132 mL |
| 5 mM | 0.6185 mL | 3.0925 mL | 6.1851 mL | 12.3701 mL | 15.4626 mL |
| 10 mM | 0.3093 mL | 1.5463 mL | 3.0925 mL | 6.1851 mL | 7.7313 mL |
| 50 mM | 0.0619 mL | 0.3093 mL | 0.6185 mL | 1.237 mL | 1.5463 mL |
| 100 mM | 0.0309 mL | 0.1546 mL | 0.3093 mL | 0.6185 mL | 0.7731 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Rucaparib, also named as AG-014699 or PF-01367338, is a poly (ADP ribose) polymerase (PARP) inhibitor. PARP is a DNA damage-activated nuclear enzyme that has a key signaling role in the base excision repair pathway. So, rucaparib has been also found to be most effective in cells deficient in DNA repair, where the cells deficient are caused by exposure to genotoxic agents, such as irradiation produces DNA damage and its toxicity is augmented when the DNA repair is impaired. Increased radiosensitivity in presence of rucaparib was associated with persistent DNA breaks as determined by gamma-H2AX and p53BP1 foci. Rucaparib radiosensitizes prostate cancer cells, most effectively those that are PTEN-deficient and are expressing ETS gene fusion proteins, which inhibits NHEJ DNA repair.
References
Ruth Plummer, Paul Lorigan, Neil Steven, Lucy Scott, Mark R. Middleton, Richard H. Wilson, Evan Mulligan, Nicola Curtin, Diane Wang, Raz Dewji, Antonello Abbattista, Jorge Gallo, Hilary Calvert. A phase II study of the potent PARP inhibitor, Rucaparib (PF-01367338, AG014699), with temozolomide in patients with metastatic melanoma demonstrating evidence of chemopotentiation.
Payel Chatterjee, Gaurav Choudhary, Warren D. Heston, Eric A. Klein, Alex Almasan. The PARP inhibitor rucaparib radiosensitizes prostate cancer cells, most effectively those that are PTEN-deficient and are expressing ETS gene fusion proteins, which inhibit NHEJ DNA repair. Cancer Research. 2012. 72: B27.
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