Rucaparib (AG-014699,PF-01367338)

Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM for PARP1, also showing binding affinity to eight other PARP domains. Phase 1/2.

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Rucaparib (AG-014699,PF-01367338) Chemical Structure

Rucaparib (AG-014699,PF-01367338) Chemical Structure
Molecular Weight: 421.36

Validation & Quality Control

Customer Reviews(2)

Quality Control & MSDS

Related Compound Libraries

Rucaparib (AG-014699,PF-01367338) is available in the following compound libraries:

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Product Information

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  • Research Area

Product Description

Biological Activity

Description Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM for PARP1, also showing binding affinity to eight other PARP domains. Phase 1/2.
Targets PARP
IC50 1.4 nM (Ki) [1]
In vitro 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. [1] [2] 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. [3] Rucaparib inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilised D283Med cells. [4]
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. [4] 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. [5]
Features The first PARP inhibitor used in clinical trials combined with temozolomide.

Protocol(Only for Reference)

Kinase Assay: [1]

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.
Inhibition of PARP activity Inhibition of PARP activity in 5 × 103 D283Med cells is measured using various concentrations of Rucaparib (0-1 μM), compared with DMSO-only. Maximally stimulated PARP activity is measured in samples of permeabilised cells by immunological detection of the amount of poly(ADP-ribose) (PAR) formed, using the 10H anti-PAR antibody, during a 6-min incubation with NAD+ and oligonucleotide (substrate and activator). A PAR standard curve using a GCLP-validated assay is used as reference for the assay. [4]

Cell Assay: [4]

Cell lines D425Med, D283Med and D384Med cells
Concentrations 0.4 μM
Incubation Time 3 or 5 days
Method Medulloblastoma cell lines are seeded in 96-well plates at a density of 1 × 103, 3 × 103 and 3 × 103, respectively. At 24 hours (D384Med) or 48 hours (D283Med and D425Med) after seeding, the cells are exposed to various concentrations of temozolomide in the presence or absence of 0.4 μM Rucaparib. After 3 days (D425Med and D384Med) or 5 days (D283Med) of culture, cell viability is evaluated by a XTT cell proliferation kit assay. Cell growth is expressed as a percentage in relation to DMSO or 0.4 μM Rucaparib-alone controls. The concentration of temozolomide, alone or in combination with Rucaparib that inhibited growth by 50% (GI50) is calculated. The potentiation factor 50 (PF50) is defined as the ratio of the GI50 of temozolomide in the presence of Rucaparib to the GI50 of temozolomide alone.

Animal Study: [4]

Animal Models CD-1 nude mice bearing established D283Med xenografts
Dosages 1 mg/kg
Administration One or four daily by i.p.
Solubility 30% propylene glycol, 5% Tween 80, 65% D5W, 30 mg/mL


Clinical Trial Information( data from

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT00664781 Recruiting brca1 Mutation Carrier|brca2 Mutation Carrier|Breast Cancer|Ovarian Cancer Cancer Research UK 2007-12 Phase 2
NCT01009190 Recruiting Advanced Solid Tumors Clovis Oncology, Inc. 2010-02 Phase 1
NCT01482715 Recruiting Metastatic Solid Tumor|Breast Cancer|Ovarian Cancer Clovis Oncology, Inc. 2011-11 Phase 1|Phase 2

Chemical Information

Download Rucaparib (AG-014699,PF-01367338) SDF
Molecular Weight (MW) 421.36


CAS No. 459868-92-9
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Syonnyms AG-014447
Solubility (25°C) * In vitro DMSO 84 mg/mL (199 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% propylene glycol, 5% Tween 80, 65% D5W, 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 8-fluoro-5-(4-((methylamino)methyl)phenyl)-3,4-dihydro-2H-azepino[5,4,3-cd]indol-1(6H)-one phosphoric acid

Preparing Stock Solutions

Stock Solution (1ml DMSO) 1mM 10mM 20mM 30mM
Mass(mg) 0.42136 4.2136 8.4272 12.6408

Research Area

Customer Reviews (2)

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Source J Biol Chem, 2012, 287(47), 39824-33. Rucaparib (AG-014699,PF-01367338) purchased from Selleck
Method Western Blotting
Cell Lines HaCaT cells
Concentrations 1 μM
Incubation Time 30 min
Results preincubation of purified PARP-1 with AG-014699, a potent PARP inhibitor , prior to PARP-1 activation led to decreased associa-tion between PARP-1 and XPA.

Click to enlarge
Source Dr David Schürmann from University of Basel. Rucaparib (AG-014699,PF-01367338) purchased from Selleck
Method Kruskal-Wallis and the post-hoc Dunn’s Multiple Comparison tests, immuno-staining
Cell Lines Primary human lung fibroblast cells (MRC-5)
Concentrations 0-1 μM
Incubation Time 2 h

Product Citations (8)

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    Features:Most potent and selective PARPi reported thus far.

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  • Rucaparib (AG-014699,PF-01367338)

    Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM for PARP1, also showing binding affinity to eight other PARP domains. Phase 1/2.

    Features:The first PARP inhibitor used in clinical trials combined with temozolomide.

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