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/ PARP / Rucaparib phosphate

瑞卡帕布磷酸盐 /Rucaparib phosphate 99%+

货号：A424427 同义名： 芦卡帕利 / PF-01367338 phosphate;AG-014699 phosphate Ambeed 开学季，买赠积分，赢豪礼

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： 99%+
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, EC50: 1 nM

PARP1, Ki: 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

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
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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