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Rucaparib

产品编号 T4463 CAS 283173-50-2

别名: AG-14447, PF-01367338, 瑞卡帕布, AG014699

Rucaparib (PF-01367338) 是一种口服有效的 PARP 蛋白抑制剂，对 PARP-1 的 Ki 为 1.4 nM。它是六磷酸己糖脱氢酶 (H6PD) 抑制剂，有用于去势抵抗性前列腺癌 (CRPC) 的研究潜力。

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Rucaparib, CAS 283173-50-2

规格	价格/CNY	货期
1 mg	￥ 266	现货
2 mg	￥ 378	现货
5 mg	￥ 622	现货
10 mg	￥ 996	现货
25 mg	￥ 1,780	现货
50 mg	￥ 2,890	现货
100 mg	￥ 4,330	现货
200 mg	￥ 6,180	现货
500 mg	￥ 9,360	现货
1 mL * 10 mM (in DMSO)	￥ 683	现货

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其他形式的 Rucaparib:

选择批次

纯度: 99.89%

纯度: 99.01%

纯度: 98.37%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Rucaparib (PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, and also shows binding affinity to eight other PARP.
靶点活性	PARP1:1.4 nM
体外活性	Rucaparib is the most potent PARP inhibitor in enzyme assays (Ki, 1.4 nM), and a possible N-demethylation metabolite of AG14644. 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
体内活性	Rucaparib and AG14584 significantly (P < 0.05) increases temozolomide toxicity. Rucaparib (1 mg/kg) significantly increases temozolomide-induced body weight loss. Rucaparib (0.1 mg/kg) results in a 50% increase in the temozolomide-induced tumor growth delay. Rucaparib 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
激酶实验	Inhibition of PARP activity in 5×103 D283Med cells is measured using various concentrations of Rucaparib (0-1 μM), compared with DMSO-only. Maximally stimulated PARP activity is measured in samples of permeabilised cells by immunologica.
细胞实验	Medulloblastoma cell lines are seeded in 96-well plates at a density of 1×103, 3×103 and 3×103, respectively. At 24 hours (D384Med) or 48 hours (D283Med and D425Med) after seeding, the cells are exposed to various concentrations of temozolomide in the presence or absence of 0.4 μM Rucaparib. After 3 days (D425Med and D384Med) or 5 days (D283Med) of culture, cell viability is evaluated by a XTT cell proliferation kit assay. Cell growth is expressed as a percentage in relation to DMSO or 0.4 μM Rucaparib-alone controls. The concentration of temozolomide, alone or in combination with Rucaparib that inhibited growth by 50% (GI50) is calculated. The potentiation factor 50 (PF50) is defined as the ratio of the GI50 of temozolomide in the presence of Rucaparib to the GI50 of temozolomide alone.
动物实验	Rucaparib is formulated in saline.A single dose of temozolomide is administrated p.o. as a suspension in saline at 200 mg/kg either alone or in combination with a single i.p. administration of PARP inhibitor administered at 0.1 [Rucaparib and MS-AG14644 (equivalent to 0.078 mg/kg free AG14644 only)], 1.0, and 10 mg/kg (for the mesylate salts equivalent to 0.79 and 7.9 mg/kg free AG14451 and AG14452 and 0.78 and 7.8 free AG14531 and AG14644). Control animals are treated with either normal saline p.o. and i.p or normal saline p.o and PARP inhibitor 10 mg/kg i.p.

别名	AG-14447, PF-01367338, 瑞卡帕布, AG014699
分子量	323.36
分子式	C19H18FN3O
CAS No.	283173-50-2

存储

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

溶解度

DMSO: 32.5 mg/mL (100.5 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.0925 mL	15.4626 mL	30.9253 mL	77.3132 mL
	5 mM	0.6185 mL	3.0925 mL	6.1851 mL	15.4626 mL
	10 mM	0.3093 mL	1.5463 mL	3.0925 mL	7.7313 mL
	20 mM	0.1546 mL	0.7731 mL	1.5463 mL	3.8657 mL
	50 mM	0.0619 mL	0.3093 mL	0.6185 mL	1.5463 mL
	100 mM	0.0309 mL	0.1546 mL	0.3093 mL	0.7731 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Thomas HD,etal.Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial.Mol Cancer Ther. 2007 Mar;6(3):945-56. 2. Hunter JE,etal.NF-κB mediates radio-sensitization by the PARP-1 inhibitor, AG-2014699.Oncogene. 2012 Jan 12;31(2):251-64. 3. Daniel RA,etal.Central nervous system penetration and enhancement of temozolomide activity in childhood medulloblastoma models by poly(ADP-ribose) polymerase inhibitor AG-014699.Br J Cancer. 2010 Nov 9;103(10):1588-96. 4. Daniel RA,etal.Inhibition of poly(ADP-ribose) polymerase-1 enhances temozolomide and topotecan activity against childhood neuroblastoma.Clin Cancer Res. 2009 Feb 15;15(4):1241-9.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Rucaparib 283173-50-2 Chromatin/Epigenetic DNA Damage/DNA Repair PARP BRCA2 Capan-1 SSB repair PF 01367338 inhibit PF01367338 AG 14447 AG14447 poly ADP ribose polymerase AG14644 NF-κB BRCA1 H6PD AG-14447 PF-01367338 瑞卡帕布 Inhibitor AG 014699 AG014699 AG-014699 MX-1 inhibitor

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Rucaparib

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords