Rucaparib (AG014699) monocamsylate 是一种口服有效的 PARP 蛋白 (PARP-1, PARP-2 and PARP-3) 抑制剂，对 PARP-1 的 K_i 为 1.4 nM。Rucaparib monocamsylate 是六磷酸己糖脱氢酶 (H6PD) 抑制剂。Rucaparib monocamsylate 具有用于去势抵抗性前列腺癌 (CRPC) 研究的潜力。

Rucaparib (AG014699) monocamsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a K i of 1.4 nM for PARP1. Rucaparib monocamsylate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib monocamsylate has the potential for castration-resistant prostate cancer (CRPC) research.

Solid

PARP-1 1.4 nM (Ki) PARP-2

Rucaparib (AG014699) monocamsylate is a possible N-demethylation metabolite of AG14644.
Rucaparib (0.1, 1, 10, 100 μM; 24 hours) monocamsylate is cytotoxic and has the LC50 being 5?μM in Capan-1 (BRCA2 mutant) cells and only 100?nM in MX-1 (BRCA1 mutant) cells.
The radio-sensitization by Rucaparib monocamsylate is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib monocamsylate can target NF-κB activated by DNA damage and overcome toxicity observed with classical NF-κB inhibitors without compromising other vital inflammatory functions.
Rucaparib monocamsylate inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilised D283Med cells.
has not independently confirmed the accuracy of these methods. They are for reference

Rucaparib (AG014699) monocamsylate and AG14584 significantly increase Temozolomide toxicity. Rucaparib (1 mg/kg) monocamsylate significantly increases Temozolomide-induced body weight loss. Rucaparib (0.1 mg/kg) monocamsylate results in a 50% increase in the temozolomide-induced tumor growth delay.
Rucaparib (10?mg/kg for i.p. or 50, 150 mg/kg for p.o.; daily for 5 days per week for 6 weeks) monocamsylate significantly inhibits the growth of the tumor, and there is one complete tumor regression and two persistent partial regressions.
Rucaparib (150?mg/kg; p.o.; once per week for 6 weeks or three times per week for 6 weeks) monocamsylate has greatest antitumor effect with three complete regressions.
Rucaparib monocamsylate enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[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]. J Murray, et al. Tumour cell retention of rucaparib, sustained PARP inhibition and efficacy of weekly as well as daily schedules. Br J Cancer. 2014 Apr 15;110(8):1977-84.

In Vitro: DMSO : 83.33 mg/mL (149.97 mM; Need ultrasonic)配制储备液