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/ PARP / Veliparib/维利帕尼

Veliparib/维利帕尼 {[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/维利帕尼 化学结构 CAS号：912444-00-9
Veliparib/维利帕尼 化学结构
CAS号：912444-00-9
Veliparib/维利帕尼 3D分子结构
CAS号：912444-00-9
Veliparib/维利帕尼 化学结构 CAS号：912444-00-9
Veliparib/维利帕尼 3D分子结构 CAS号：912444-00-9
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Veliparib/维利帕尼 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:

全球学术期刊中引用的产品

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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

 		98%
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

 		97%
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。

Veliparib/维利帕尼 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/维利帕尼 细胞实验

Cell Line
Concentration Treated Time Description References
MDA-MB-436 10-50 µM 72 hours To evaluate the sensitivity of breast cancer cell lines to the PARP inhibitor ABT-888, results showed that only BRCA1-deficient MDA-MB-436 cells were sensitive to ABT-888. Cancer Sci. 2011 Oct;102(10):1882-8.
RWPE-1 20uM 3 days To evaluate the effect of SAHA and veliparib alone or in combination on the viability of normal prostate epithelial cells. Results showed no significant toxicity to normal cells. J Exp Clin Cancer Res. 2018 Jul 16;37(1):153.
DU145 20uM 3 days To evaluate the effect of SAHA and veliparib alone or in combination on cell viability. Results showed that co-treatment significantly decreased cell viability. J Exp Clin Cancer Res. 2018 Jul 16;37(1):153.
C4–2 20uM 3 days To evaluate the effect of SAHA and veliparib alone or in combination on cell viability. Results showed that co-treatment significantly decreased cell viability. J Exp Clin Cancer Res. 2018 Jul 16;37(1):153.
LNCaP 20uM 3 days To evaluate the effect of SAHA and veliparib alone or in combination on cell viability. Results showed that co-treatment significantly decreased cell viability. J Exp Clin Cancer Res. 2018 Jul 16;37(1):153.
KKU-055 cells 0.1-100 μM 96 h To evaluate the synergistic cytotoxic effects of BET inhibitors combined with PARP inhibitors in CCA cells, results showed that all combinations exhibited synergy. Cancer Lett. 2020 Jan 1;468:48-58.
KKU-100 cells 0.1-100 μM 96 h To evaluate the synergistic cytotoxic effects of BET inhibitors combined with PARP inhibitors in CCA cells, results showed that all combinations exhibited synergy. Cancer Lett. 2020 Jan 1;468:48-58.
U2OS 10 μM 24 h To evaluate the effect of Veliparib on DNA replication fork stability, results showed that Veliparib treatment increased the interaction between TIM and PARP1, indicating impaired TIM degradation. Cell Rep. 2024 Mar 26;43(3):113845.
SH-SY5Y cells 10 µM 24 h Veliparib effectively inhibited PARP activity and significantly restored TOM40 protein levels while reducing α-Syn protein levels. Cell Death Dis. 2024 Dec 18;15(12):914.
U2-OS cells 10 µM 25 h Veliparib treatment led to a significant increase in micronuclei formation in U2-OS cells following HU treatment, indicating that Veliparib increases genomic instability under replication stress. J Cell Biol. 2014 Aug 18;206(4):493-507.
MCF7GFP-IBD cells 10 μM 1 h Veliparib combined with ionizing radiation (IR) suppressed colony formation in irradiated MCF7GFP-IBD cells compared with IR alone, similar to the activity of the PARP1/2 inhibitor veliparib, a well established radiosensitizer. Mol Cancer Ther. 2018 Feb;17(2):407-418.
B16.SIY cells 25 μM 1 h Veliparib significantly delayed DSB repair in B16.SIY cells after 6 Gy, with persistent damage reaching that of 12 Gy or 6 Gy plus 10 μM veliparib. Mol Cancer Ther. 2018 Feb;17(2):407-418.

Veliparib/维利帕尼 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice DU145 xenograft model SAHA intraperitoneal injection, veliparib oral gavage 25 mg/kg/d 3 continuous weeks To validate the antitumor effect of SAHA and veliparib co-treatment. Results showed that co-treatment significantly inhibited tumor growth. J Exp Clin Cancer Res. 2018 Jul 16;37(1):153.
Mice B16.SIY tumor model Oral 10 mg/kg Once daily for 5 days Veliparib along with 15 Gy displayed increased tumor tissue destruction, increased DNA damage, decreased cellular proliferation, and enhanced senescence, and significantly delayed tumor growth. Mol Cancer Ther. 2018 Feb;17(2):407-418.
Mice Triple-negative breast cancer xenograft model Oral 20 mg/kg, 60 mg/kg Three times daily for three days To evaluate the penetration and distribution of Veliparib in triple-negative breast cancer xenograft models, results showed that Veliparib penetration in tumors was highly heterogeneous and positively correlated with platinum adduct formation Breast Cancer Res. 2017 Sep 11;19(1):107

Veliparib/维利帕尼 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/维利帕尼 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/维利帕尼 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/维利帕尼 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/维利帕尼 技术信息

CAS号912444-00-9
分子式C13H16N4O
分子量 244.29
SMILES Code O=C(C1=C2NC([C@]3(C)NCCC3)=NC2=CC=C1)N
MDL No. MFCD16661059
别名 ABT-888; NSC 737664
运输蓝冰
InChI Key JNAHVYVRKWKWKQ-CYBMUJFWSA-N
Pubchem ID 11960529
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

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

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