Rucaparib Phosphate

SKU: orb1301050

Description

Rucaparib Phosphate

Research Area

Epigenetics & Chromatin, Molecular Biology

Images & Validation

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Key Properties

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CAS Number	459868-92-9
MW	421.36
Purity	99.37%
Formula	C₁₉H₁₈FN₃O·H₃PO₄
SMILES	OP(O)(O)=O.CNCc1ccc(cc1)-c1[nH]c2cc(F)cc3C(=O)NCCc1c23
Target	PARP
Solubility	DMSO:78 mg/mL (185.11 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.75 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

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Target IC50	PARP:1.4 nM (Ki, cell free)
In Vivo	When 10 mg/kg Rucaparib 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, Rucaparib also significantly increased temozolomide-induced body weight loss . At 1mg/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 . Read more...
In Vitro	AG14447 (the phosphate salt of Rucaparib) is the most potent PARP inhibitor in enzyme assays (Ki: 1.4 nmol/L) . 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 . 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 . Read more...
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 . Read more...
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 . Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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MX-1, PARP, H6PD, BRCA1, Capan-1, AG 014699, AG 014699 Phosphate, AG14644, AG014699 Phosphate, AG-014699 phosphate, AG014699, BRCA2, poly ADP ribose polymerase, PF01367338, PF01367338 Phosphate, PF-01367338 phosphate, PF 01367338, PF 01367338 Phosphate, Rucaparib, Rucaparib Phosphate, SSB

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Compound Identifiers

PubChem CID

9931953 ↗

Key Properties

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No computed properties available.

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