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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:1859053-21-6
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
Rucaparib CAMSYLATE (AG014699; AG14447; PF01367338; trade name: Rubraca), the CAMSYLATE salt of rucaparib, is a potent PARP inhibitor approved by FDA for the treatment of ovarian cancer. It inhibits PARP1 with a Ki of 1.4 nM in a cell-free assay.
理化性质和储存条件
Molecular Weight (MW)555.67
FormulaC29H34FN3O5S
CAS No.1859053-21-6 (Rucaparib camsylate)
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥ 100 mg/mL
Water: N/A
Ethanol: N/A
SMILESFC1=CC2=C3C(CCNC2=O)=C(C4=CC=C(CNC)C=C4)NC3=C1.O=S(C[C@@]5(C6(C)C)C(C[C@@]6([H])CC5)=O)(O)=O
SynonymsAG014699 camsylate; PF-01367338; AG 014699; PF 01367338 camsylate; AG-014699; PF01367338; AG-14447 camsylate; AG 14447; AG14447 camsylate; Trade name: Rubraca
实验参考方法
In Vitro

In vitro activity: Rucaparib is a potent inhibitor of purified full-length human PARP-1 and shows higher inhibition of cellular PARP in LoVo and SW620 cells. Besides, Rucaparib binds detectably to eight other PARP domains, including PARP2, 3, 4, 10, 15, 16, TNKS1 and TNKS2. The radio-sensitization by Rucaparib is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib could 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.


Kinase Assay: Inhibition of human full-length recombinant PARP-1 by [32P]NAD+ incorporation is measured. The [32P]ADP-ribose incorporated into acid insoluble material is quantified using a PhosphorImager. Ki is calculated by nonlinear regression analysis.


Cell Assay: In the MDCKII parental cell line, which overexpressed human (h) ABCB1, both apically and basolaterally directed translocation of rucaparib were the same. Treatment of the cells with the ABCB1 inhibitor zosuquidar resulted in a slight decrease in apically directed transport, which could be either due to a specific inhibition of an unidentified rucaparib uptake transporter at the basolateral side, or inhibition of endogenous canine ABCB1. The result shown that rucaparib is a transported substrate of ABCB1.

In VivoRucaparib is not toxic but significantly enhances temozolomide-induced TGD in the DNA repair protein-competent D384Med xenografts. Pharmacokinetics studies also show that Rucaparib is detected in the brain tissue, which indicates that Rucaparib has potential in intra-cranial malignancy therapy. Rucaparib significantly potentiates the cytotoxicity of topotecan and temozolomide in NB-1691, SH-SY-5Y, and SKNBE (2c) cells. Rucaparib enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts.
Animal modelCD-1 nude mice bearing established D283Med xenografts
Formulation & DosageDissolved in saline; 1 mg/kg; One or four daily by i.p.
References

Mol Cancer Ther. 2007 Mar;6(3):945-56; Br J Cancer. 2010 Nov 9;103(10):1588-96; Clin Cancer Res. 2009 Feb 15;15(4):1241-9.