Rucaparib camsylate(Synonyms: AG014699 camsylate; PF-01367338 camsylate)

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Rucaparib camsylate (Synonyms: AG014699 camsylate; PF-01367338 camsylate)

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。

Rucaparib camsylate(Synonyms: AG014699 camsylate; PF-01367338 camsylate)

Rucaparib camsylate Chemical Structure

CAS No. : 1327258-57-0

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Rucaparib camsylate 的其他形式现货产品:

Rucaparib monocamsylate

生物活性

Rucaparib (AG014699) camsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib camsylate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib camsylate has the potential for castration-resistant prostate cancer (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 LC50 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 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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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.

参考文献
  • [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.

    [3]. Matt Shirley, et al. Rucaparib: A Review in Ovarian Cancer. Target Oncol. 2019 Apr;14(2):237-246.

    [4]. Jianneng Li, et al. Hexose-6-phosphate dehydrogenase blockade reverses prostate cancer drug resistance in xenograft models by glucocorticoid inactivation. Sci Transl Med. 2021 May 26;13(595):eabe8226.

    [5]. Hunter JE, et al. NF-κB mediates radio-sensitization by the PARP-1 inhibitor, AG-014699. Oncogene, 2012, 31(2), 251-264.

    [6]. 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.

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