Rucaparib (AG-014699,PF-01367338) phosphate
Molecular Weight(MW): 421.36
Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3.
Cited by 35 Publications
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Choose Selective PARP Inhibitors
|Description||Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3.|
|Features||The first PARP inhibitor used in clinical trials combined with temozolomide.|
Rucaparib is a potent inhibitor of purified full-length human PARP-1 and shows higher inhibition of cellular PARP in LoVo and SW620 cells. Besides, Rucaparib binds detectably to eight other PARP domains, including PARP2, 3, 4, 10, 15, 16, TNKS1 and TNKS2.   The radio-sensitization by Rucaparib is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib could target NF-κB activated by DNA damage and overcome toxicity observed with classical NF-κB inhibitors without compromising other vital inflammatory functions.  Rucaparib inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilised D283Med cells. 
|In vivo||Rucaparib is not toxic but significantly enhances temozolomide-induced TGD in the DNA repair protein-competent D384Med xenografts. Pharmacokinetics studies also show that Rucaparib is detected in the brain tissue, which indicates that Rucaparib has potential in intra-cranial malignancy therapy.  Rucaparib significantly potentiates the cytotoxicity of topotecan and temozolomide in NB-1691, SH-SY-5Y, and SKNBE (2c) cells. Rucaparib enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts. |
Ki Determination:Inhibition of human full-length recombinant PARP-1 by [32P]NAD+ incorporation is measured. The [32P]ADP-ribose incorporated into acid insoluble material is quantified using a PhosphorImager. Ki is calculated by nonlinear regression analysis.
-  Thomas HD, et al. Mol Cancer Ther, 2007, 6(3), 945-956.
-  Kotz, J. SciBX 5(13); doi:10.1038/scibx.2012.323.
-  Hunter JE, et al. Oncogene, 2012, 31(2), 251-264.
|In vitro||DMSO||84 mg/mL (199.35 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03954366||Recruiting||Drug: Rucaparib|Drug: Rosuvastatin|Drug: Oral Contraceptives||Neoplasms||Clovis Oncology Inc.||May 8 2019||Phase 1|
|NCT03824704||Recruiting||Drug: Rucaparib|Drug: Nivolumab||Epithelial Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Carcinoma|High Grade Serous Carcinoma|Endometrioid Adenocarcinoma||Clovis Oncology Inc.|Bristol-Myers Squibb|Foundation Medicine||May 15 2019||Phase 2|
|NCT03413995||Recruiting||Drug: Rucaparib||Prostate Cancer Metastatic||Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Clovis Oncology Inc.||September 10 2018||Phase 2|
|NCT03572478||Recruiting||Drug: Rucaparib|Drug: Nivolumab||Prostate Cancer|Endometrial Cancer||University of Chicago|Bristol-Myers Squibb|Clovis Oncology Inc.||August 14 2018||Phase 1|Phase 2|
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