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Purity: ≥98%
Rucaparib (formerly AG-014699 or PF-01367338; trade name: Rubraca) is a potent, tricyclic indole based, and orally bioavailable inhibitor of PARP (poly(ADP-Ribose) polymerase) with potential anticancer activity. In cell-free experiments, it inhibits PARP1 with a Ki of 1.4 nM. The US FDA approved rucaparib in December 2016 for the treatment of ovarian cancer in women. Rucaparib binds specifically to PARP1 and prevents PARP1 from repairing damaged DNA, which increases the number of breaks in DNA strands and encourages apoptosis and genomic instability. This could reverse tumor cell resistance to chemotherapy and radiation therapy and increase the cytotoxicity of agents that damage DNA.
| Targets |
PARP-1 ( Ki = 1.4 nM )
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
The amount of [32P]NAD+ incorporation-induced inhibition of human full-length recombinant PARP-1 is measured. With a PhosphorImager, the amount of [32P]ADP-ribose added to acid-insoluble material is measured. The nonlinear regression analysis is used to calculate Ki.
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| Cell Assay |
The density of medulloblastoma cell lines is plated at 1 × 103, 3 × 103, and 3 × 103 in 96-well plates, in that order. Cells are seeded and exposed to different concentrations of temozolomide with or without 0.4 μM Rucaparib at 24, 48, or 72 hours later (D283Med and D425Med). Utilizing an XTT cell proliferation kit assay, cell viability is assessed following 3 days (D425Med and D384Med) or 5 days (D283Med) of culture. In comparison to DMSO or 0.4 μM Rucaparib-alone controls, the percentage of cell growth is given. One can compute the growth inhibition by 50% (GI50) of temozolomide, either in isolation or in conjunction with Rucaparib. The ratio of the GI50 of temozolomide in the presence of Rucaparib to the GI50 of temozolomide alone is known as the potentiation factor 50 (PF50).
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| Animal Protocol |
Female athymic nude mice, implanted SW620 colorectal tumor cells (1 × 107 cells per animal) s.c.
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 IP, single dose for 0.1 mg/kg and 10 mg/kg, five daily doses for 0-0.5 mg/kg |
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| References |
| Molecular Formula |
C19H18FN3O.H3PO4
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| Molecular Weight |
421.36
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| Exact Mass |
323.14
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| CAS # |
459868-92-9
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| Related CAS # |
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| Appearance |
Light yellow solid powder
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| SMILES |
CNCC1=CC=C(C=C1)C2=C3CCNC(=O)C4=C3C(=CC(=C4)F)N2.OP(=O)(O)O
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| InChi Key |
FCCGJTKEKXUBFZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H18FN3O.H3O4P/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;1-5(2,3)4/h2-5,8-9,21,23H,6-7,10H2,1H3,(H,22,24);(H3,1,2,3,4)
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| Chemical Name |
6-fluoro-2-[4-(methylaminomethyl)phenyl]-3,10-diazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13)-tetraen-9-one;phosphoric acid
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| Synonyms |
AG014699; PF-01367338; AG 014699; PF 01367338; AG-014699; PF01367338; AG-14447; AG 14447; AG14447; Trade name: Rubraca; Rucaparib
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3733 mL | 11.8663 mL | 23.7327 mL | |
| 5 mM | 0.4747 mL | 2.3733 mL | 4.7465 mL | |
| 10 mM | 0.2373 mL | 1.1866 mL | 2.3733 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03552471 | Active Recruiting |
Drug: Rucaparib Camsylate Other: Pharmacokinetic Study |
BRCA1 Gene Mutation BRCA2 Gene Mutation |
Ohio State University Comprehensive Cancer Center |
July 12, 2018 | Phase 1 |
| NCT03442556 | Active Recruiting |
Drug: Rucaparib Camsylate Drug: Rucaparib |
ATM Gene Mutation PSA Progression |
University of Washington | August 24, 2018 | Phase 2 |
AG-014699 inhibits Single strand break (SSB) repair to a similar extent regardless of cellular NF-κB status.Oncogene, 2012, 31(2), 251-264. |
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