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Rucaparib

Catalog No. T4463   CAS 283173-50-2
Synonyms: AG-14447, PF-01367338, AG014699

Rucaparib (PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, and also shows binding affinity to eight other PARP.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Rucaparib Chemical Structure
Rucaparib, CAS 283173-50-2
Pack Size Availability Price/USD Quantity
2 mg In stock $ 41.00
5 mg In stock $ 67.00
10 mg In stock $ 117.00
25 mg In stock $ 183.00
50 mg In stock $ 247.00
100 mg In stock $ 383.00
200 mg In stock $ 568.00
500 mg In stock $ 915.00
1 mL * 10 mM (in DMSO) In stock $ 74.00
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Purity: 99.89%
Purity: 99.01%
Purity: 98.37%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Rucaparib (PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, and also shows binding affinity to eight other PARP.
Targets&IC50 PARP1:1.4 nM
In vitro Rucaparib is the most potent PARP inhibitor in enzyme assays (Ki, 1.4 nM), and a possible N-demethylation metabolite of AG14644. 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 and AG14584 significantly (P < 0.05) increases temozolomide toxicity. Rucaparib (1 mg/kg) significantly increases temozolomide-induced body weight loss. Rucaparib (0.1 mg/kg) results in a 50% increase in the temozolomide-induced tumor growth delay. 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
Kinase Assay 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 immunologica.
Cell Research 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 Research Rucaparib is formulated in saline.A single dose of temozolomide is administrated p.o. as a suspension in saline at 200 mg/kg either alone or in combination with a single i.p. administration of PARP inhibitor administered at 0.1 [Rucaparib and MS-AG14644 (equivalent to 0.078 mg/kg free AG14644 only)], 1.0, and 10 mg/kg (for the mesylate salts equivalent to 0.79 and 7.9 mg/kg free AG14451 and AG14452 and 0.78 and 7.8 free AG14531 and AG14644). Control animals are treated with either normal saline p.o. and i.p or normal saline p.o and PARP inhibitor 10 mg/kg i.p.
Synonyms AG-14447, PF-01367338, AG014699
Molecular Weight 323.36
Formula C19H18FN3O
CAS No. 283173-50-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 32.5 mg/mL (100.5 mM)

TargetMolReferences and Literature

1. Thomas HD,etal.Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial.Mol Cancer Ther. 2007 Mar;6(3):945-56. 2. Hunter JE,etal.NF-κB mediates radio-sensitization by the PARP-1 inhibitor, AG-2014699.Oncogene. 2012 Jan 12;31(2):251-64. 3. Daniel RA,etal.Central nervous system penetration and enhancement of temozolomide activity in childhood medulloblastoma models by poly(ADP-ribose) polymerase inhibitor AG-014699.Br J Cancer. 2010 Nov 9;103(10):1588-96. 4. Daniel RA,etal.Inhibition of poly(ADP-ribose) polymerase-1 enhances temozolomide and topotecan activity against childhood neuroblastoma.Clin Cancer Res. 2009 Feb 15;15(4):1241-9.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Anti-Cancer Approved Drug Library Anti-Breast Cancer Compound Library Inhibitor Library Target-Focused Phenotypic Screening Library FDA-Approved Drug Library Bioactive Compound Library Anti-Pancreatic Cancer Compound Library

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Keywords

Rucaparib 283173-50-2 Chromatin/Epigenetic DNA Damage/DNA Repair PARP BRCA2 Capan-1 SSB repair PF 01367338 inhibit PF01367338 AG 14447 AG14447 poly ADP ribose polymerase AG14644 NF-κB BRCA1 H6PD AG-14447 PF-01367338 Inhibitor AG 014699 AG014699 AG-014699 MX-1 inhibitor

 

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