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Rucaparib Camsylate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Rucaparib Camsylate图片
CAS NO:1327258-57-0
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
AG014699 camsylate
PF-01367338 camsylate
产品介绍
Rucaparib (AG014699) camsylate 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Ki为 1.4 nM。Rucaparib camsylate 是六磷酸己糖脱氢酶 (H6PD) 抑制剂。Rucaparib camsylate 具有用于去势抵抗性前列腺癌 (CRPC) 研究的潜力。
生物活性

Rucaparib (AG014699) camsylate is an orally active, potent inhibitor ofPARPproteins (PARP-1, PARP-2 and PARP-3) with aKiof 1.4 nM forPARP1. Rucaparib camsylate is a modesthexose-6-phosphate dehydrogenase (H6PD)inhibitor. Rucaparib camsylate has the potential for castration-resistant prostatecancer(CRPC) research[1][2][3][4].

IC50& Target

PARP-1

1.4 nM (Ki)

PARP-2

 

PARP-3

 

体外研究
(In Vitro)

Rucaparib (AG014699) camsylate is a possible N-demethylation metabolite of AG14644[1].
Rucaparib (0.1, 1, 10, 100 μM; 24 hours) camsylate is cytotoxic and has the LC50being 5 μM in Capan-1 (BRCA2 mutant) cells and only 100 nM in MX-1 (BRCA1 mutant) cells[2].
The radio-sensitization by Rucaparib camsylate is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib camsylate 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 camsylate inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilised D283Med cells[6].

体内研究
(In Vivo)

Rucaparib (AG014699) camsylate and AG14584 significantly increase Temozolomide toxicity. Rucaparib (1 mg/kg) camsylate significantly increases Temozolomide-induced body weight loss. Rucaparib (0.1 mg/kg) camsylate results 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) camsylate 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) camsylate has greatest antitumor effect with three complete regressions[2].
Rucaparib camsylate enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts[6].

Animal Model:Female CD-1 nude mice aged 10-12 weeks with Capan-1 cells[2]
Dosage:10 mg/kg or 50, 150 mg/kg
Administration:10 mg/kg for i.p. or 50, 150 mg/kg for p.o.
Result:Significantly inhibited the growth of the tumor.
Clinical Trial
Formula

C19H18FN3O.xC10H16O4S

CAS 号

1327258-57-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.