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Rucaparib Phosphate

Catalog No. T6127   CAS 459868-92-9
Synonyms: AG-014699 phosphate, PF-01367338, AG-014699, PF-01367338 phosphate

Rucaparib Phosphate (PF-01367338 phosphate) is an inhibitor of PARP (Ki: 1.4 nM for PARP1) that is used in clinical therapy to sensitize cancer cells to chemotherapy.

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Rucaparib Phosphate Chemical Structure
Rucaparib Phosphate, CAS 459868-92-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 32.00
2 mg In stock $ 45.00
5 mg In stock $ 72.00
10 mg In stock $ 117.00
25 mg In stock $ 198.00
50 mg In stock $ 261.00
100 mg In stock $ 413.00
200 mg In stock $ 615.00
1 mL * 10 mM (in DMSO) In stock $ 72.00
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Purity: 99.1%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Rucaparib Phosphate (PF-01367338 phosphate) is an inhibitor of PARP (Ki: 1.4 nM for PARP1) that is used in clinical therapy to sensitize cancer cells to chemotherapy.
Targets&IC50 PARP:1.4 nM (Ki, cell free)
In vitro AG14447 (the phosphate salt of Rucaparib) is the most potent PARP inhibitor in enzyme assays (Ki: 1.4 nmol/L) [1]. In permeabilised D283Med cells, Rucaparib (AG-014699), at concentrations of 0.1, 0.4 and 1?μ inhibited PARP-1 activity by 81.1, 96.8 and 97.1%, respectively [2]. AG014699 (≤10 μM) was cytotoxic to cells with mutated BRCA1/2 or XRCC3 and to UACC3199 cells with epigenetically silenced BRCA1 but not to cells without BRCA1/2 or XRCC3 mutations or that were heterozygous for BRCA2 mutation [3].
In vivo When 10 mg/kg AG14447 was administered in combination with temozolomide, body weight loss was observed at days 4 to 13 posttreatment with the nadir body weight ranging from 83% to 96% of the starting weight. At a dose of 1 mg/kg, AG14447 also significantly increased temozolomide-induced body weight loss [1]. At 1?mg/kg daily five times, AG-014699 alone did not cause any marked toxicity or affect tumour growth compared with vehicle-only controls. Co-administration of AG-014699 with temozolomide also resulted in complete tumour regressions in all mice, of which three out of five were sustained throughout the experiment. The MMR-defective D283Med xenografts grew very rapidly and showed very little response to temozolomide alone (TGD of only 2 days) with no regressions observed in any mice [2].
Kinase Assay We measured inhibition of human full-length recombinant PARP-1 by [32P]NAD+ incorporation as described previously. The [32P]ADP-ribose incorporated into acid insoluble material was quantified using a PhosphorImager. Kis were calculated by nonlinear regression analysis [1].
Cell Research Inhibition of PARP activity in 5000 exponentially growing D283Med cells was measured following treatment with a range of AG-014699 concentrations (0–1?μ), in comparison with DMSO-only controls. Maximally stimulated PARP activity was measured in replicate samples (n?3) of permeabilised cells by immunological detection of the amount of poly(ADP-ribose) (PAR) formed, using 10H anti-PAR antibody, during a 6-min incubation with NAD+ and oligonucleotide (substrate and activator) by reference to a PAR standard curve using a GCLP-validated assay described previously [2].
Animal Research One or four daily doses of PARP inhibitor AG-014699 (1?mg/kg intraperitoneally (i.p.)) were given to CD-1 nude mice bearing established D283Med xenografts. At 0.5, 2, 6 and 24?h after the initial or fourth daily dose of AG-014699, three animals per time point were bled by cardiac puncture under general anaesthesia, and then killed. Plasma was separated from the blood samples using standard methods and stored at ?80°C. The brains and tumours were removed, snap frozen in liquid nitrogen and stored at ?80°C before analysis. Blood, tumour and brain tissue were removed from three untreated control animals and processed in the same way [2].
Synonyms AG-014699 phosphate, PF-01367338, AG-014699, PF-01367338 phosphate
Molecular Weight 421.36
Formula C19H18FN3O·H3PO4
CAS No. 459868-92-9

Storage

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

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 78 mg/mL (185.1 mM)

TargetMolReferences and Literature

1. Thomas HD, et al. Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial. Mol Cancer Ther, 2007, 6(3), 945-956. 2. Daniel RA, et al. 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, 103(10), 1588-1596. 3. Drew Y, et al. Therapeutic potential of poly(ADP-ribose) polymerase inhibitor AG014699 in human cancers with mutated or methylated BRCA1 or BRCA2. J Natl Cancer Inst. 2011 Feb 16;103(4):334-46.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Cancer Approved Drug Library Clinical Compound Library Fluorochemical Library FDA-Approved & Pharmacopeia Drug Library Anti-Cancer Compound Library FDA-Approved Drug Library DNA Damage & Repair Compound Library

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Keywords

Rucaparib Phosphate 459868-92-9 Chromatin/Epigenetic DNA Damage/DNA Repair PARP BRCA2 BRCA1 inhibit Capan-1 AG-014699 phosphate PF 01367338 AG-014699 Phosphate AG 014699 Phosphate MX-1 repair PF-01367338 Rucaparib AG14644 AG014699 Phosphate SSB NF-κB H6PD PF01367338 Phosphate poly ADP ribose polymerase PF 01367338 Phosphate AG-014699 AG014699 AG 014699 Inhibitor PF-01367338 phosphate PF-01367338 Phosphate PF01367338 inhibitor

 

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