Rucaparib monocamsylate

SKU: orb1307769

Description

Rucaparib camsylate is a potent PARP inhibitor with a Ki of 1.4 nM for PARP1 and affinity for eight other PARP family members. It is widely used in vitro and in vivo for cancer research, particularly in studies of BRCA-deficient tumors and synthetic lethality.

Research Area

Epigenetics & Chromatin, Molecular Biology

Images & Validation

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Key Properties

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CAS Number	1859053-21-6
MW	555.66
Purity	99.82%
Formula	C₂₉H₃₄FN₃O₅S
SMILES	[H][C@@]12CC[C@@](CS(O)(=O)=O)(C(=O)C1)C2(C)C.CNCc1ccc(cc1)-c1[nH]c2cc(F)cc3C(=O)NCCc1c23
Target	PARP
Solubility	DMSO:82.33 mg/mL (148.17 mM);10% DMSO+40% PEG300+5% Tween-80+45% Saline:3.3 mg/mL (5.94 mM)

Bioactivity

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Target IC50	PARP1:1.4 nM (Ki)
In Vivo	Rucaparib is not toxic but obviously enhances temozolomide-induced TGD in the DNA repair protein-competent D384Med xenografts. Rucaparib and AG14584 obviously (P < 0.05) increase temozolomide toxicity. Rucaparib enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts. Rucaparib significantly potentiates the cytotoxicity of topotecan and temozolomide in NB-1691, SH-SY-5Y, and SKNBE (2c) cells. 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. Pharmacokinetics studies also show that Rucaparib is detected in the brain tissue, which indicates that Rucaparib has potential in intra-cranial malignancy therapy . Read more...
In Vitro	Rucaparib is the most effective PARP inhibitor in enzyme assays (Ki: 1.4 nM). Rucaparib inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilized D283Med cells. Rucaparib could target NF-κB activated by DNA damage and overcome toxicity observed with classical NF-κB inhibitors without compromising other vital inflammatory functions. The radio-sensitization by Rucaparib is due to downstream inhibition of activation of NF-κB and is independent of SSB repair inhibition . 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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BRCA2, Capan-1, BRCA1, AG14644, AG014699 monocamsylate, inhibit, MX-1, PARP, PARP1, PARP-1, NF-κB, poly ADP ribose polymerase, Inhibitor, H6PD, SSB, repair, Rucaparib Camsylate, Rucaparib monocamsylate, PF-01367338 monocamsylate

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Compound Identifiers

PubChem CID

121490161 ↗

Key Properties

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No computed properties available.

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