1327258-57-0
1327258-57-0 structure
- Name: Rucaparib camsylate
- Chemical Name: Rucaparib camsylate
- CAS Number: 1327258-57-0
- Molecular Formula: C19H18FN3O.xC10H16O4S
- Molecular Weight:
- Catalog: Signaling Pathways Cell Cycle/DNA Damage PARP
- Create Date: 2022-08-16 12:02:44
- Modify Date: 2024-01-11 11:55:01
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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].
| Name | Rucaparib camsylate |
|---|
| Description | 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]. |
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| Related Catalog | |
| Target |
PARP-1:1.4 nM (Ki) PARP-2 PARP-3 |
| 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]. |
| 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. |
| References |
[3]. Matt Shirley, et al. Rucaparib: A Review in Ovarian Cancer. Target Oncol. 2019 Apr;14(2):237-246. |
| Molecular Formula | C19H18FN3O.xC10H16O4S |
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