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/ PARP / Rucaparib phosphate

瑞卡帕布磷酸盐 /Rucaparib phosphate {[allProObj[0].p_purity_real_show]}

货号：A424427 同义名： 芦卡帕利 / PF-01367338 phosphate;AG-014699 phosphate

Rucaparib phosphate is an inhibitor of PARP with Ki of 1.4 nM for PARP1, also showing binding affinity to eight other PARP domains.

Rucaparib phosphate 化学结构 CAS号：459868-92-9
Rucaparib phosphate 化学结构
CAS号：459868-92-9
Rucaparib phosphate 3D分子结构
CAS号：459868-92-9
Rucaparib phosphate 化学结构 CAS号：459868-92-9
Rucaparib phosphate 3D分子结构 CAS号：459868-92-9
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Rucaparib phosphate 纯度/质量文件 产品仅供科研

货号：A424427 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 PARP ↓ PARP1 ↓ PARP2 ↓ PARP3 ↓ 其他靶点 纯度
PJ34 HCl ++

PARP, EC50: 20 nM

 		99%+
Rucaparib phosphate ++++

PARP, Ki: 1.4 nM

 		99%+
3-Aminobenzamide ++

PARP, IC50: <50 nM

 		98%
AZD-2461 ✔ 99%+
BGP-15 ✔ 99%+
NU1025 +

PARP, IC50: 400 nM

 		97%
Benzamide +

PARP, IC50: 3.3 μM

 		98%
Picolinamide +

PARP, IC50: 95 μM

 		98%
AG14361 +++

PARP1, Ki: <5 nM

 		98+%
Iniparib ✔ 98%
Talazoparib ++++

PARP1, IC50: 0.57 nM

 		99%+
NMS-P118 ++

PARP1, Kd: 0.009 μM

 		98+%
UPF 1069 +

PARP1, IC50: 8.0 μM

 		++

PARP2, IC50: 0.3 μM

 		98%
A-966492 ++++

PARP1, Ki: 1 nM

PARP1, EC50: 1 nM

 		+++

PARP2, Ki: 1.5 nM

 		99%+
Veliparib ++

PARP1, Ki: 5.2 nM

 		+++

PARP2, Ki: 2.9 nM

 		98%
Niraparib tosylate +++

PARP1, IC50: 3.8 nM

 		+++

PARP2, IC50: 2.1 nM

 		99%+
Stenoparib ++++

PARP1, IC50: 1 nM

 		++++

PARP2, IC50: 1.2 nM

 		98%
Olaparib +++

PARP1, IC50: 5 nM

 		++++

PARP2, IC50: 1 nM

 		98%
Niraparib +++

PARP1, IC50: 3.8 nM

 		+++

PARP2, IC50: 2.1 nM

 		98%
ME0328 +

PARP1, IC50: 6.3 μM

 		+

PARP3, IC50: 0.89 μM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Rucaparib phosphate 生物活性

靶点

  • PARP

    PARP, Ki:1.4 nM
描述 PARP1, also called as Poly (ADP-ribose) polymerase, is involved in the signaling of DNA damage. It can recognize and bind DNA single or double-strand breaks, thus possessing various cellular function, including regulation of apoptosis and chromosome stability, gene amplification and transcription, as well as cell division and differentiation. Rucaparib Phosphate is a potent PARP inhibitor with Ki value of 1.4 nM (measured by enzyme assays)[1]. Rucaparib Phosphate at dose ranging in 1-10 μM can suppress the level of PAR, as well as induce γ-H2AX, formation and PARP cleavage in a dose-dependent manner indicative of DNA damage and apoptosis, respectively, in MDA-MB468, MDA-MB-231, and Cal-51 cells in the presence of 5% FBS-supplemented DMEM medium for 72 h. Rucaparib Phosphate at concentrations >2.5 μM decreased the p-Stat3 in MDA-MB-468 and MDA-MB-231, as well as dose-dependently increased the p-Akt-S473 in MDA-MB-468 and Cal-51 cells[2]. Rucaparib Phosphate can chemosensitize neuroblastoma cell lines to temozolomide or topotecan in vitro and in vivo. Rucaparib Phosphate at concentration of 0.4 μM caused a significant sensitization of topotecan (1-30 nM) and temozolomide (1-200 μM) in NB-1691, SH-SY-5Y and SKNBE(2c) cells. Rucaparib Phosphate (1 mg/kg) increased the temozolomide-induced (68 mg/kg) tumor growth delay by 50% (to >89 days) and complete and increased the number of mice with complete and persistent tumor regressions (‎≥ 100 days). Co-administration of Rucaparib Phosphate (1 mg/kg) with topotecan (1 mg/kg) increased total number of complete regressions[3].
作用机制 Rucaparib Phosphate can compete with NAD+ for the PARP catalytic site[4]

Rucaparib phosphate 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
A2780 Growth Inhibition Assay IC50=3.94 ± 0.25 μM 23729402
A549 400 nM Growth Inhibition Assay 24 h increases cellular radiosensitivity 24411611
AU565 500 nM Growth Inhibition Assay 10–15 d reduces cell growth in the four lines and significantly 25128455
BT474 500 nM Growth Inhibition Assay 10–15 d reduces cell growth in the four lines and significantly 25128455

Rucaparib phosphate 动物研究

Dose Mice: 2 mg/kg - 150 mg/kg[5] (p.o.), 0.05 mg/kg - 10 mg/kg[1] (i.p.) Rat: 15 mg/kg[5] (i.v.)
Administration p.o., i.p., i.v.
Pharmacokinetics
Animal Mice[5] Rats[5] Dogs[5] Monkeys[5]
Dose 15 mg/kg 15 mg/kg 15 mg/kg 15 mg/kg
Administration p.o. i.v. i.v. i.v.
AUC0→inf 718 ng·h/ml
Vd 6.5 L/kg 15.2 L/kg 7.2 L/kg
T1/2 2.93 h 3.5 h 4.5 h 5.2 h
Vz/F 88300 ml/kg
CL 45.3 ml/min/kg 61.8 ml/min/kg 33.8 ml/min/kg
Cmax 173 ng/ml
AUC0→∞ 5.7 μg·h/ml 4.1 μg·h/ml 7.4 μg·h/ml
CL/F 20900 ml/h/kg
AUC0→t 682 ng·h/ml

Rucaparib phosphate 参考文献

[1]Thomas HD, Calabrese CR, et al. Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial. Mol Cancer Ther. 2007 Mar;6(3):945-56.

[2]Chuang HC, Kapuriya N, et al. Differential anti-proliferative activities of poly(ADP-ribose) polymerase (PARP) inhibitors in triple-negative breast cancer cells. Breast Cancer Res Treat. 2012 Jul;134(2):649-59.

[3]Daniel RA, Rozanska AL, et al. 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.

[4]Javle M, Curtin NJ, et al. The potential for poly (ADP-ribose) polymerase inhibitors in cancer therapy. Ther Adv Med Oncol. 2011 Nov;3(6):257-67.

[5]RUBRACA

Rucaparib phosphate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.37mL

0.47mL

0.24mL

11.87mL

2.37mL

1.19mL

23.73mL

4.75mL

2.37mL

Rucaparib phosphate 技术信息

CAS号459868-92-9
分子式C19H21FN3O5P
分子量 421.359
别名 芦卡帕利 ;PF-01367338 phosphate;AG-014699 phosphate;PF-01367338;AG-014699;Rucaparib (phosphate)
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature
溶解度

DMSO: 35 mg/mL(83.06 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 5 mg/mL(11.87 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方

IP 2% DMSO+water 9 mg/mL clear

PO 0.5% CMC-Na 30 mg/mL suspension

Tags: Rucaparib | 459868-92-9 | AG-014699 | PF-01367338 | PARP Inhibitor | Cell Cycle/DNA Damage | Epigenetics | PARP | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Rucaparib phosphate 纯度/质量文件 | Rucaparib phosphate 亚型比较 | Rucaparib phosphate 生物活性 | Rucaparib phosphate 细胞研究 | Rucaparib phosphate 动物研究 | Rucaparib phosphate 参考文献 | Rucaparib phosphate 实验方案 | Rucaparib phosphate 技术信息

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