化合物 Rucaparib acetate T61657

Product Introduction
Bioactivity


英文名: Rucaparib acetate

描述: Rucaparib (AG014699) acetate is a highly effective oral inhibitor of PARP proteins, specifically targeting PARP-1, PARP-2, and PARP-3, with a Ki value of 1.4 nM for PARP1. Additionally, it exhibits inhibitory action on hexose-6-phosphate dehydrogenase (H6PD) to a moderate extent. Rucaparib acetate shows promise in the field of research for castration-resistant prostate cancer (CRPC). [1] [2] [3] [4]

体外活性: Rucaparib (AG014699) acetate is a possible N-demethylation metabolite of AG14644 [1]. Rucaparib (0.1, 1, 10, 100 μM; 24 hours) acetate is cytotoxic and has the LC 50 being 5 μM in Capan-1 (BRCA2 mutant) cells and only 100 nM in MX-1 (BRCA1 mutant) cells [2]. The radio-sensitization by Rucaparib acetate is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib acetate can target NF-κB activated by DNA damage and overcome toxicity observed with classical NF-κB inhibitors without compromising other vital inflammatory functions [5]. Rucaparib acetate inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilised D283Med cells [6].

体内活性: Rucaparib (AG014699) acetate and AG14584 significantly increase Temozolomide toxicity. Rucaparib (1 mg/kg) acetate significantly increases Temozolomide-induced body weight loss. Rucaparib (0.1 mg/kg) acetate esults in a 50% increase in the temozolomide-induced tumor growth delay [1]. Rucaparib (10 mg/kg for i.p. or 50, 150 mg/kg for p.o.; daily for 5 days per week for 6 weeks) acetate significantly inhibits the growth of the tumor, and there is one complete tumor regression and two persistent partial regressions [2]. Rucaparib (150 mg/kg; p.o.; once per week for 6 weeks or three times per week for 6 weeks) acetate has greatest antitumor effect with three complete regressions [2]. Rucaparib acetate enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts [6].

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

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途