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Cat. No. M1644
AG-014699 Structure

PF-01367338, Rucaparib

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL In DMSO USD 80 In stock
10mg USD 107 In stock
50mg USD 295 In stock
200mg USD 750 In stock
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Quality Control
Biological Activity

AG-014699 (PF-01367338, Rucaparib) is a PARP inhibitor with a Ki of 1.4 nM. AG-014699 is the phosphate salt of AG 014447 (CAS 283173-50-2) and has improved aqueous solubility. Poly (ADP-ribose) polymerases (PARPs) are activated by DNA single- and double-strand breaks and promote repair of DNA damage through the relaxation of chromatin and recruitment of other repair proteins. AG-014699 inactivates PARP activity in cells with homologous recombination DNA repair pathway mutations at LC50 values ranging from 1.3-5.5 μM. Radio-sensitization by AG-014699 is due to downstream inhibition of NF-κB activation, and independent of SSB repair inhibition. Although AG014699 can enhance response to some chemotherapeutic drugs via improved delivery, this does not apply to doxorubicin. PARP inhibitors may still be of use to counter doxorubicin toxicity.

Customer Product Validations & Biological Datas
Source Oncogene (2012). Figure 2. AG-014699
Method Cytotoxicity Assay
Cell Lines p65+/+ and p65−/− MEFs
Concentrations 0.1 μM
Incubation Time 48 h
Results Here we show that, co-incubation with either AG-014699, p65 siRNA or PARP-1 siRNA radio-sensitized p65+/+ MEFs 1.4-fold compared to mock-transfected cells treated with IR. Significantly, a combination of p65 siRNA and AG-014699 showed no further sensitization
Source Oncogene (2012). Figure 1. AG-014699
Method Western blots
Cell Lines p65+/+ and p65−/− MEFs
Concentrations 0.1 μM
Incubation Time 48 h
Results Cells treated with AG-014699, or a combination of AG-014699 and p65 siRNA exhibited very low (< 5%) PARP activity
Cell Experiment
Cell lines LoVo and SW620 cells
Preparation method We estimated cell growth inhibition in exponentially growing LoVo and SW620 cells in 96-well plates exposed to increasing concentrations of single-agent PARP inhibitor, temozolomide or topotecan, or combinations of temozolomide or topotecan with PARP inhibitor for 5 days before staining with sulforhodamine B as described previously (18). Cell growth, determined after subtraction of time 0 values, was expressed as a percentage of the relevant DMSO, cytotoxic drug, or PARP inhibitor alone control, as appropriate. GI50 (concentration of drug that inhibited growth by 50%) values were calculated from the computer-generated curves (GraphPad Software, Inc. San Diego CA).
Concentrations 0~1000µM
Incubation time 5 days
Animal Experiment
Animal models SW620 tumor xenografts
Formulation saline
Dosages 0.1, 1, 10mg/kg
Administration oral
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 421.36
Formula C19H18FN3O.H3PO4
CAS Number 459868-92-9
Purity 100.00%
Solubility DMSO ≥40 mg/mL
Storage at -20°C

Differential anti-proliferative activities of poly(ADP-ribose) polymerase (PARP) inhibitors in triple-negative breast cancer cells.
Chuang et al. Breast Cancer Res Treat. 2012 Jul;134(2):649-59. PMID: 22678161.

The clinically active PARP inhibitor AG014699 ameliorates cardiotoxicity but does not enhance the efficacy of doxorubicin, despite improving tumor perfusion and radiation response in mice.
Ali et al. Mol Cancer Ther. 2011 Dec;10(12):2320-9. PMID: 21926192.

NF-κB mediates radio-sensitization by the PARP-1 inhibitor, AG-014699.
Hunter et al. Oncogene. 2012 Jan 12;31(2):251-64. PMID: 21706052.

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Keywords: AG-014699, PF-01367338, Rucaparib supplier, PARP, inhibitors

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