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Purity: ≥98%
Rucaparib CAMSYLATE (AG014699;AG14447; PF01367338; trade name:Rubraca), theCAMSYLATE salt of rucaparib, is a potent PARP inhibitor approved by FDA for the treatment of ovarian cancer. In a test without cells, it inhibits PARP1 with a Ki of 1.4 nM.
| Targets |
PARP-1 ( Ki = 1.4 nM ); PARP-2; PARP-3
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|---|---|
| ln Vitro |
In vitro activity: Rucaparib (AG014699) camsylate is a possible N-demethylation metabolite of AG14644[1].
Rucaparib (0.1, 1, 10, 100 μM; 24 hours) camsylate is cytotoxic; in Capan-1 (BRCA2 mutant) cells, its LC50 is 5 μM, while in MX-1 (BRCA1 mutant) cells, it is only 100 nM[2]. Rucaparib camsylate induces radiosensitization independent of SSB repair inhibition, as it results from downstream inhibition of NF-κB activation. Without impairing other essential inflammatory functions, rucaparib camsylate can target NF-κB that is activated by DNA damage and overcome the toxicity seen with classical NF-κB inhibitors[5]. Rucaparib camsylate inhibits PARP-1 activity in permeabilized D283Med cells by 97.1% at a concentration of 1 μM[6]. |
| ln Vivo |
Rucaparib camsylate and AG14584 significantly increase Temozolomide toxicity. Temozolomide-induced body weight loss is markedly enhanced by rucaparib (1 mg/kg) camsylate. The temozolomide-induced tumor growth delay is increased by 50% when rucaparib (0.1 mg/kg) camsylate is used[1]. Rucaparib (10 mg/kg intraperitoneally or 50–150 mg/kg po; daily, five days a week, for six weeks) There is one complete tumor regression and two persistent partial tumor regressions as a result of camsylate's strong tumor growth inhibition[2]. The most potent antitumor effect is achieved with three complete regressions when rutaparib (150 mg/kg; p.o. ; once weekly for 6 weeks or three times weekly for 6 weeks) is used for camsylate[2]. Rucaparib camsylate in NB1691 and SHSY5Y xenografts shows complete and sustained tumor regression and improves the antitumor activity of temozolomide[6].
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| Enzyme Assay |
It is measured how much [32P]NAD+incorporation inhibits human full-length recombinant PARP-1. A PhosphorImager is used to quantify the [32P]ADP-ribose that is integrated into acid-insoluble material. Nonlinear regression analysis is used to calculate Kiis.
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| Cell Assay |
The following day, the cells were treated with escalating drug concentrations after being seeded into 24-well plates (2,500–4000 cells/well). After 72–96 hours, cell viability was evaluated by adding CellTiter-Glo reagent and utilizing a plate reader to measure luminescence. Cells were seeded in 6-well plates in triplicate (500–4000 cells/well) for clonogenic survival assays. Following plating, cells were given a drug treatment 16–18 hours later and were left to grow for 14 days.
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| Animal Protocol |
CD-1 nude mice bearing established D283Med xenografts; Dissolved in saline;1 mg/kg;One or four daily by i.p.
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| References |
| Molecular Formula |
C29H34FN3O5S
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|---|---|
| Molecular Weight |
555.67
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| CAS # |
1859053-21-6
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| Related CAS # |
459868-92-9 (phosphate); 1859053-21-6 (Rucaparib camsylate); 283173-50-2
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| Appearance |
Solid powder
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| SMILES |
CC1([C@@H]2CC[C@]1(C(=O)C2)CS(=O)(=O)O)C.CNCC1=CC=C(C=C1)C2=C3CCNC(=O)C4=C3C(=CC(=C4)F)N2
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| InChi Key |
INBJJAFXHQQSRW-STOWLHSFSA-N
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| InChi Code |
InChI=1S/C19H18FN3O.C10H16O4S/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;1-9(2)7-3-4-10(9,8(11)5-7)6-15(12,13)14/h2-5,8-9,21,23H,6-7,10H2,1H3,(H,22,24);7H,3-6H2,1-2H3,(H,12,13,14)/t;7-,10-/m.1/s1
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| Chemical Name |
[(1S,4R)-7,7-dimethyl-2-oxo-1-bicyclo[2.2.1]heptanyl]methanesulfonic acid;6-fluoro-2-[4-(methylaminomethyl)phenyl]-3,10-diazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13)-tetraen-9-one
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| Synonyms |
AG014699 camsylate; PF-01367338; AG 014699; PF 01367338 camsylate; AG-014699; PF01367338; AG-14447 camsylate; AG 14447; AG14447 camsylate; Trade name: Rubraca
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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 |
| 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) |
DMSO: ≥ 100 mg/mL
Water: N/A Ethanol: N/A |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.74 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.74 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.74 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7996 mL | 8.9981 mL | 17.9963 mL | |
| 5 mM | 0.3599 mL | 1.7996 mL | 3.5993 mL | |
| 10 mM | 0.1800 mL | 0.8998 mL | 1.7996 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 |
| NCT03442556 | Active Recruiting |
Drug: Rucaparib Camsylate Drug: Rucaparib |
ATM Gene Mutation PSA Progression |
University of Washington | August 24, 2018 | Phase 2 |
| 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 |
| NCT04455750 | Active Recruiting |
Drug: Rucaparib camsylate Drug: Enzalutamide |
Stage IV Prostate Cancer AJCC v8 Stage IVA Prostate Cancer AJCC v8 |
Alliance for Clinical Trials in Oncology |
February 19, 2021 | Phase 3 |
| NCT03521037 | Active Recruiting |
Drug: Rucaparib camsylate | Neoplasms | pharmaand GmbH | February 27, 2018 | Phase 1 |
| NCT02986100 | Completed | Drug: C-14 labeled Rucaparib Drug: Rucaparib |
Solid Tumor | pharmaand GmbH | November 2016 | Phase 1 |
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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