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/ PARP / Veliparib

维利帕尼 /Veliparib {[allProObj[0].p_purity_real_show]}

货号：A164131 同义名： ABT-888;NSC 737664

Veliparib（ABT-888）是一种强效的PARP抑制剂，抑制PARP1和PARP2的Ki值分别为5.2 nM和2.9 nM。

Veliparib 化学结构 CAS号：912444-00-9
Veliparib 化学结构
CAS号：912444-00-9
Veliparib 3D分子结构
CAS号：912444-00-9
Veliparib 化学结构 CAS号：912444-00-9
Veliparib 3D分子结构 CAS号：912444-00-9
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Veliparib 纯度/质量文件 产品仅供科研

货号：A164131 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。

Veliparib 生物活性

靶点

  • PARP1

    PARP1, Ki:5.2 nM

  • PARP2

    PARP2, Ki:2.9 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. PARP-2 is the closest homolog of PARP1 (~62% similarity in catalytic domain) and compensates for PARP-1 activity in DNA single-strand break. Veliparib is a potent PARP inhibitor with Ki values of 5.2nM and 2.9nM for PARP-1 and PARP-2 (measured by recombinant human PARP), respectively[1], which has shown promise in combination with chemotherapy in preclinical studies. In presence of 5μM Veliparib for 15, 30 and 240 min, the level of PAR protein, the product catalyzed by PARP, was dramatically decreased by Veliparib in both irradiated and non-irradiated H460 lung cancer cells to nearly undetectable levels. 10-fold decrease in cell survival at 6Gy irradiation can be observed 8 days latere after treatment with 5μM Veliparib for 6h and then washed off. At 6h after 5Gy irradiation, the addition of 5μM Veliparib significantly increased the percentage of cells containingγ-H2AX foci, a marker of double-stranded DNA breaks. 3Gy irradiation combined with 5μM Veliparib showed a 2.8-fold increase in apoptosis, whereas Veliparib alone showed no increase in apoptosis and 3 Gy irradiation increased apoptosis 2-fold. Similar pattern of increase in autophagic cells can be seen. Treatment with Veliparib, 25mg/kg, i.p., for 5 consecutive days improved tumor growth delay in nude mice implanted H460 tumors[2]. Significant inhibition in the level of PAR can be observed in B16F10 flank tumor xenograft mice dosed with Veliparib (25 and 3.125 mg/kg/d, p.o., b.i.d. x 2) with or without temozolomide, which showed the inhibition by Veliparib on PARP activity in vivo[1].
作用机制 Veliparib more favorably interacts with the space between Gln319 and Glu322 in PARP-2 over the Glu763 and Asp766 in PARP-1 in the catalytic domain.[3]

Veliparib 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
697 Growth Inhibition Assay IC50=29.0235 μM SANGER
A2780 Growth Inhibition Assay IC50=30.7457 μM SANGER
A388 Growth Inhibition Assay IC50=21.9091 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=43.5691 μM SANGER

Veliparib 动物研究

Dose Mice: 5 mg/kg, 25 mg/kg[6] (p.o.), 100 mg/kg[5] (diet), 25 mg/kg[2] (i.p.)
Administration p.o., i.p.

Veliparib 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00770471 Brain and Central Nervous Syst... 展开 >>em Tumors 收起 << Phase 1 Completed - United States, Alabama ... 展开 >> UAB Comprehensive Cancer Center Birmingham, Alabama, United States, 35294-3410 United States, California UCSF Helen Diller Family Comprehensive Cancer Center San Francisco, California, United States, 94115 United States, Georgia Winship Cancer Institute of Emory University Atlanta, Georgia, United States, 30322 United States, Maryland Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins Baltimore, Maryland, United States, 21231 United States, Massachusetts Massachusetts General Hospital Boston, Massachusetts, United States, 02114 United States, Michigan Josephine Ford Cancer Center at Henry Ford Hospital Detroit, Michigan, United States, 48202 United States, North Carolina Wake Forest University Comprehensive Cancer Center Winston-Salem, North Carolina, United States, 27157-1096 United States, Ohio Cleveland Clinic Taussig Cancer Center Cleveland, Ohio, United States, 44195 United States, Pennsylvania Abramson Cancer Center of the University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104-4283 UPMC Cancer Centers Pittsburgh, Pennsylvania, United States, 15232 United States, Wisconsin University of Wisconsin Comprehensive Cancer Center Madison, Wisconsin, United States, 53792-6164 收起 <<
NCT00526617 Non-hematologic Malignancies ... 展开 >> Metastatic Melanoma Breast Cancer Ovarian Cancer Primary Peritoneal Cancer Fallopian Tube Cancer Hepatocellular Carcinoma 收起 << Phase 1 Completed - -
NCT01419548 Neoplasms Phase 1 Withdrawn - United States, Maryland ... 展开 >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 United States, Pennsylvania University of Pittsburgh Cancer Center Pittsburgh, Pennsylvania, United States 收起 <<

Veliparib 参考文献

[1]Donawho CK, Luo Y, et al. ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models. Clin Cancer Res. 2007 May 1;13(9):2728-37.

[2]Albert JM, Cao C, et al. Inhibition of poly(ADP-ribose) polymerase enhances cell death and improves tumor growth delay in irradiated lung cancer models. Clin Cancer Res. 2007 May 15;13(10):3033-42.

[3]Steffen JD, Brody JR, et al. Structural Implications for Selective Targeting of PARPs. Front Oncol. 2013 Dec 20;3:301.

[4]Kinders RJ, Hollingshead M, et al. Preclinical modeling of a phase 0 clinical trial: qualification of a pharmacodynamic assay of poly (ADP-ribose) polymerase in tumor biopsies of mouse xenografts. Clin Cancer Res. 2008;14(21):6877-85.

[5]To C, Kim EH, et al. The PARP inhibitors, veliparib and olaparib, are effective chemopreventive agents for delaying mammary tumor development in BRCA1-deficient mice. Cancer Prev Res (Phila). 2014;7(7):698-707.

Veliparib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.09mL

0.82mL

0.41mL

20.47mL

4.09mL

2.05mL

40.94mL

8.19mL

4.09mL

Veliparib 技术信息

CAS号912444-00-9
分子式C13H16N4O
分子量 244.29
别名 ABT-888;NSC 737664
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature
溶解度

DMSO: 30 mg/mL(122.8 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
动物实验配方

0.5% methylcellulose+0.2% Tween 80+water 5 mg/mL suspension

Tags: Veliparib | ABT-888;NSC 737664 | PARP | AmBeed-信号通路专用抑制剂 | Veliparib 纯度/质量文件 | Veliparib 亚型比较 | Veliparib 生物活性 | Veliparib 细胞研究 | Veliparib 动物研究 | Veliparib 临床数据 | Veliparib 参考文献 | Veliparib 实验方案 | Veliparib 技术信息

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