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Rucaparib Phosphate

产品编号 T6127 CAS 459868-92-9

别名: AG-014699 phosphate, PF-01367338, 芦卡帕利, AG-014699, 瑞卡帕布磷酸盐, PF-01367338 phosphate

Rucaparib Phosphate (PF-01367338 phosphate) 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 Phosphate, CAS 459868-92-9

规格	价格/CNY	货期
1 mg	￥ 258	现货
2 mg	￥ 365	现货
5 mg	￥ 622	现货
10 mg	￥ 995	现货
25 mg	￥ 1,780	现货
50 mg	￥ 2,890	现货
100 mg	￥ 4,330	待询
200 mg	￥ 6,180	待询
1 mL * 10 mM (in DMSO)	￥ 658	现货

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其他形式的 Rucaparib Phosphate:

选择批次

纯度: 99.1%

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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 Phosphate (PF-01367338 phosphate) is an inhibitor of PARP (Ki: 1.4 nM for PARP1) that is used in clinical therapy to sensitize cancer cells to chemotherapy.
靶点活性	PARP:1.4 nM (Ki, cell free)
体外活性	AG14447 (the phosphate salt of Rucaparib) is the most potent PARP inhibitor in enzyme assays (Ki: 1.4 nmol/L) [1]. In permeabilised D283Med cells, Rucaparib (AG-014699), at concentrations of 0.1, 0.4 and 1?μ inhibited PARP-1 activity by 81.1, 96.8 and 97.1%, respectively [2]. AG014699 (≤10 μM) was cytotoxic to cells with mutated BRCA1/2 or XRCC3 and to UACC3199 cells with epigenetically silenced BRCA1 but not to cells without BRCA1/2 or XRCC3 mutations or that were heterozygous for BRCA2 mutation [3].
体内活性	When 10 mg/kg AG14447 was administered in combination with temozolomide, body weight loss was observed at days 4 to 13 posttreatment with the nadir body weight ranging from 83% to 96% of the starting weight. At a dose of 1 mg/kg, AG14447 also significantly increased temozolomide-induced body weight loss [1]. At 1?mg/kg daily five times, AG-014699 alone did not cause any marked toxicity or affect tumour growth compared with vehicle-only controls. Co-administration of AG-014699 with temozolomide also resulted in complete tumour regressions in all mice, of which three out of five were sustained throughout the experiment. The MMR-defective D283Med xenografts grew very rapidly and showed very little response to temozolomide alone (TGD of only 2 days) with no regressions observed in any mice [2].
激酶实验	We measured inhibition of human full-length recombinant PARP-1 by [32P]NAD+ incorporation as described previously. The [32P]ADP-ribose incorporated into acid insoluble material was quantified using a PhosphorImager. Kis were calculated by nonlinear regression analysis [1].
细胞实验	Inhibition of PARP activity in 5000 exponentially growing D283Med cells was measured following treatment with a range of AG-014699 concentrations (0–1?μ), in comparison with DMSO-only controls. Maximally stimulated PARP activity was measured in replicate samples (n?3) of permeabilised cells by immunological detection of the amount of poly(ADP-ribose) (PAR) formed, using 10H anti-PAR antibody, during a 6-min incubation with NAD+ and oligonucleotide (substrate and activator) by reference to a PAR standard curve using a GCLP-validated assay described previously [2].
动物实验	One or four daily doses of PARP inhibitor AG-014699 (1?mg/kg intraperitoneally (i.p.)) were given to CD-1 nude mice bearing established D283Med xenografts. At 0.5, 2, 6 and 24?h after the initial or fourth daily dose of AG-014699, three animals per time point were bled by cardiac puncture under general anaesthesia, and then killed. Plasma was separated from the blood samples using standard methods and stored at ?80°C. The brains and tumours were removed, snap frozen in liquid nitrogen and stored at ?80°C before analysis. Blood, tumour and brain tissue were removed from three untreated control animals and processed in the same way [2].

别名	AG-014699 phosphate, PF-01367338, 芦卡帕利, AG-014699, 瑞卡帕布磷酸盐, PF-01367338 phosphate
分子量	421.36
分子式	C19H18FN3O·H3PO4
CAS No.	459868-92-9

存储

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

溶解度

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 78 mg/mL (185.1 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	2.3733 mL	11.8663 mL	23.7327 mL	59.3317 mL
	5 mM	0.4747 mL	2.3733 mL	4.7465 mL	11.8663 mL
	10 mM	0.2373 mL	1.1866 mL	2.3733 mL	5.9332 mL
	20 mM	0.1187 mL	0.5933 mL	1.1866 mL	2.9666 mL
	50 mM	0.0475 mL	0.2373 mL	0.4747 mL	1.1866 mL
	100 mM	0.0237 mL	0.1187 mL	0.2373 mL	0.5933 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, et al. Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial. Mol Cancer Ther, 2007, 6(3), 945-956. 2. Daniel RA, et al. 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, 103(10), 1588-1596. 3. Drew Y, et al. Therapeutic potential of poly(ADP-ribose) polymerase inhibitor AG014699 in human cancers with mutated or methylated BRCA1 or BRCA2. J Natl Cancer Inst. 2011 Feb 16;103(4):334-46.

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 Phosphate 459868-92-9 Chromatin/Epigenetic DNA Damage/DNA Repair PARP BRCA2 BRCA1 inhibit Capan-1 AG-014699 phosphate PF 01367338 AG-014699 Phosphate AG 014699 Phosphate MX-1 repair PF-01367338 Rucaparib 芦卡帕利 AG14644 AG014699 Phosphate SSB NF-κB H6PD PF01367338 Phosphate poly ADP ribose polymerase PF 01367338 Phosphate AG-014699 AG014699 AG 014699 Inhibitor 瑞卡帕布磷酸盐 PF-01367338 phosphate PF-01367338 Phosphate PF01367338 inhibitor

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Rucaparib Phosphate

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