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Rucaparib monocamsylate

Catalog No. T16807 CAS 1859053-21-6

Synonyms: Rucaparib Camsylate

Rucaparib monocamsylate (Rucaparib Camsylate) is a PARP inhibitor (PARP1,Ki of 1.4 nM). Rucaparib Camsylate also displays binding affinity to eight other PARP domains.

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Rucaparib monocamsylate Chemical Structure

Rucaparib monocamsylate, CAS 1859053-21-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 55.00
10 mg	In stock	$ 97.00
25 mg	In stock	$ 163.00
50 mg	In stock	$ 247.00
100 mg	In stock	$ 372.00
200 mg	In stock	$ 549.00
1 mL * 10 mM (in DMSO)	In stock	$ 68.00

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Purity: 99.8%

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Description	Rucaparib monocamsylate (Rucaparib Camsylate) is a PARP inhibitor (PARP1,Ki of 1.4 nM). Rucaparib Camsylate also displays binding affinity to eight other PARP domains.
Targets&IC50	PARP1:1.4 nM (Ki)
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 [1][2][3].
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 [1][3][4].

Synonyms	Rucaparib Camsylate
Molecular Weight	555.66
Formula	C29H34FN3O5S
CAS No.	1859053-21-6

Storage

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

Solubility Information

DMSO: 82.33 mg/mL(148.17 mM)

References 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. Hunter JE, et al. NF-κB mediates radio-sensitization by the PARP-1 inhibitor, AG-014699. Oncogene, 2012, 31(2), 251-264. 3. 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. 4. Daniel RA, et al. Inhibition of poly(ADP-ribose) polymerase-1 enhances temozolomide and topotecan activity against childhood neuroblastoma. Clin Cancer Res, 2009, 15(4), 1241-1249.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Approved Drug Library Drug Repurposing Compound Library EMA Approved Drug Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Inhibitor Library Anti-Cancer Drug Library Anti-Pancreatic Cancer Compound Library Approved Drug Library FDA-Approved & Pharmacopeia Drug Library

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Keywords

Rucaparib monocamsylate 1859053-21-6 Chromatin/Epigenetic DNA Damage/DNA Repair PARP repair H6PD BRCA1 poly ADP ribose polymerase AG14644 SSB PF-01367338 monocamsylate Capan-1 Inhibitor AG014699 monocamsylate NF-κB inhibit MX-1 BRCA2 Rucaparib Camsylate inhibitor

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