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Rucaparib

CAS No. : 283173-50-2

MCE 國際站：Rucaparib

產(chǎn)品活性：Rucaparib (AG014699) 是一種口服有效的 PARP 蛋白 (PARP-1, PARP-2 and PARP-3) 抑制劑，對 PARP-1 的 K_i 為 1.4 nM。Rucaparib 是六磷酸己糖脫氫酶 (H6PD) 抑制劑。Rucaparib 具有用于去勢抵抗性前列腺癌 (CRPC) 研究的潛力。

研究領域：Cell Cycle/DNA Damage  |  Epigenetics

作用靶點：PARP

In Vitro: Rucaparib (AG014699) is a possible N-demethylation metabolite of AG14644.
Rucaparib (0.1, 1, 10, 100 μM; 24 hours) 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 is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib can target NF-κB activated by DNA damage and overcome toxicity observed with classical NF-κB inhibitors without compromising other vital inflammatory functions.
Rucaparib inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilised D283Med cells.

In Vivo: Rucaparib (AG014699) and AG14584 significantly increase Temozolomide toxicity. 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.
Rucaparib (10?mg/kg for i.p. or 50, 150 mg/kg for p.o.; daily for 5 days per week for 6 weeks) 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) has greatest antitumor effect with three complete regressions.
Rucaparib enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts.

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