Veliparib (ABT-888)

For research use only. Not for use in humans.

目录号：S1004 别名： NSC 737664 中文名称：维利帕尼

CAS No. 912444-00-9

Veliparib (ABT-888, NSC 737664)是一种有效的PARP1和PARP2抑制剂，无细胞试验中K_i分别为5.2 nM和2.9 nM，对SIRT2没有活性。Veliparib 可增加自噬和凋亡。Phase 3。

规格

价格

库存

购买数量

10mM (1mL in DMSO)	RMB 1277.12	现货
10mg	RMB 973.01	现货
25mg	RMB 1859.13	现货
50mg	RMB 3010.72	现货
200mg	RMB 8108.1	现货
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客户使用Selleck生产的Veliparib (ABT-888)发表文献182篇：

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产品安全说明书

PARP抑制剂选择性比较

生物活性

产品描述

特性

ABT-888增强常见癌症疗法的效果，比如放射疗法和烷基化剂。

靶点

PARP2 ^[1] (Cell-free assay)	PARP1 ^[1] (Cell-free assay)
2.9 nM(Ki)	5.2 nM(Ki)

体外研究

ABT-888有效抑制PARP，作用于PARP-1和PARP-2时K_i值分别为5.2和2.9 nM。ABT-888降低肺癌H460细胞中克隆基因的存活率，且抑制DNA修复。^[1]ABT-888抑制C41细胞，EC50为2 nM。^[2] ABT-888和放射物联用减少肿瘤血管的形成。^[3]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
C41	MWHLbY5ie2ViQYPzZZk>		M{TzVlMxKG2rbh?=		NW\TZmZjUW6qaXLpeIlwdiCxZjDQRXJROSC5aYToJGVEPTBib3[gNE4xODJizszN	NHy5fGg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUi4PFc3OCd-MUm4PFg4PjB:L3G+
Jurkat	NEXRN3FMcW6jc3WgRZN{[Xl?		NH3xTHo6PiCq	NUf2VYg{TE2VTx?=	NFq4Z3dKdmirYnn0bY9vKG:oIGDBVnAyKGG\|c3Xzd4VlKGG\|IILl[JVkfGmxbjDv[kBk\WyuII\pZYJqdGm2eTD3bZRpKEWFNUCgc4YhOyEQvF2=	M{TlV\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OEWwNVk6Lz5{M{i1NFE6QTxxYU6=
Capan1	M4XZ[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NHrFeGM4OiCq	NXu2ZlhQTE2VTx?=	Mnr0RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDCVmNCOiCpZX7lJI12fGG2ZXSgbJVu[W5iQ3HwZY4yKGOnbHzzJJdqfGhiSVO1NEBw\iB\|OT63JO69VQ>?	MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN7OEO4N{c,OjR\|OUizPFM9N2F-
DT40	NU\lT\|hYS3m2b4TvfIlkKEG\|c3H5		M1nLZ\|czKGh?	M1e3bWROW09?	NGfUUFVEgXSxdH;4bYNqfHliYXfhbY5{fCClaHnjb4VvKEKUQ1GyMYRm\mmlaXXueEBFXDRyIHPlcIx{	NE\BTJI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmyNlU5Pyd-MkS5NlI2QDd:L3G+
ML-1	MXvBdI9xfG:2aXOgRZN{[Xl?	M{XVN\|IvPSEQvF2=	MViyOEBp	M2ewNWROW09?	M1vzU3N6dmW{Z3nzeIlk[WyueTDlcohidmOnczDUVmFKVC2rbnT1Z4VlKGGyb4D0c5NqeyCrbjDNUE0yKGOnbHzz	M{GxW\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEm1NVM2Lz5{NEi5OVE{PTxxYU6=
HCT-116	NUjodlM4U2mwYYPlJGF{e2G7	MWewMlUh\|ryP	NWT0e5A3OjRiaB?=		M{PscXBCWlBiYXP0bZZqfHliZHXjdoVie2W\|	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzB3NEKxN{c,OjNyNUSyNVM9N2F-
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A4-Fuk	NVywdI1nT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NYjheo9kUUN3ME20N{42PjlzIN88US=>	MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NFY5PzFxJ{7TRW5ITVJ:L3G+
MDA-MB-361	MlfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				M4HNZmlEPTB;NEOuPFQyPCEQvF2=	MkKxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVA3QDdzLze+V2FPT0WUPD;hQi=>
BALL-1	M2PuS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				Mn\ZTWM2OD12Mz65OVMzKM7:TR?=	NFyyO\|A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2ODZ6N{GvK\|5USU6JRWK8M4E,
T98G	NF\3[IhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NXjLfIJ{UUN3ME20OE45PTF5IN88US=>	MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NFY5PzFxJ{7TRW5ITVJ:L3G+
Mo-T	NHHnTYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NHTFWGFKSzVyPUS1MlY{QDlizszN	NFvCN\|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2ODZ6N{GvK\|5USU6JRWK8M4E,
MHH-PREB-1	MlfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				M2nLWGlEPTB;NEWuO\|U5PSEQvF2=	M4DKdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUxPjh5MT:nQnNCVkeHUkyvZV4>
ALL-PO	NFXPXVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				M{npSGlEPTB;NEeuN\|c6OSEQvF2=	M{DoV\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUxPjh5MT:nQnNCVkeHUkyvZV4>
NCI-H510A	MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MmfjTWM2OD12Nz65NFM1KM7:TR?=	MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NFY5PzFxJ{7TRW5ITVJ:L3G+
ML-2	MlHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MnnSTWM2OD12OT63PFU3KM7:TR?=	MkLhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVA3QDdzLze+V2FPT0WUPD;hQi=>

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-STAT3 / STAT3 / p-AKT(S473) / p-AKT(T308) / p-ERK / p-p38; PubMed: 22678161 Breast Cancer Res Treat Effects of AG-014699, AZD-2281, ABT-888, or BSI-201 on the phosphorylation status of Stat3, Akt, ERK, and p38 in MDA-MB-468, MDA-MB-231, and Cal-51 cells after 72 h of treatment	22678161
Immunofluorescence	HuR; PubMed: 28687616 Cancer Res Immunofluorescent images of HuR (green) in MIA PaCa-2 cells treated with PARPi for 12hr. Nuclei were stained with DAPI. Magnification 40X. BRCA1; PubMed: 21917757 Int J Oncol Effects of ABT-888 and/or bortezomib on BRCA1 and RAD51 foci formation. BRCA1 and RAD1 foci induced by ABT-888 were completely resolved in cells cotreated with bortezomib. Image acquisition was performed with an epifluorescence microscope (BX51; Olympus) and multispectral color camera (Nuance FX; CRi) with a 60× or 100× magnification lens and oil immersion.	28687616 21917757
Growth inhibition assay	Cell viability (TNBC cell lines); PubMed: 27880910 Cell Rep BRCA-proficient TNBC cell lines were treated with veliparib in the absence and presence of dinaciclib, demonstrating reduced IC50 values in the presence of dinaciclib. Cell viability (melanoma cells); PubMed: 29956724 Int J Oncol Dose-dependent inhibitory effect of ABT-888 on melanoma cell proliferation. Human melanoma cell lines were exposed to diluents (control; CTRL) or increasing concentrations of ABT-888 for 72 h and their viability was assessed by MTT assay. Absorbance was detected at 540 nm with a microplate reader and data were expressed as a percentage of the CTRL. Data are the means ± SD of 3 experiments performed in triplicate. Statistical significance was calculated against the CTRL (P<0.05; *P<0.01).	27880910 29956724

体内研究

ABT-888推迟NCI-H460 移植瘤模型的肿瘤生长。ABT-888在B16F10 和9L 移植瘤模型中抑制PARP，从而增强temozolomide的抗癌活性。^[1]ABT-888和其他细胞毒素药剂联用作用于MX-1移植瘤模型时显示出强抗癌效力。^[2]在A375和 Colo829移植瘤模型中按肿瘤大小，每千克分别加3和12.5 mg ABT-888，可以看到肿瘤内95%以上PAR被抑制。^[4]

激酶实验：^[1]	- 合并体外PARP实验: 在含有50 mM Tris (pH 为8.0), 1 mM DTT,和 4 mM MgCl₂的缓冲溶液中进行酶活性测定。PARP反应包含1.5 μM [³H]-NAD⁺ (1.6 μCi/mmol), 200 nM 生物素组蛋白 H1, 200 nM slDNA,及1 nM PARP-1或4 nM PARP-2酶。在加有100 μL 反应液的 96孔板上进行SPA检测。在50 μL含有PARP和DNA的2×酶液混合物中加入50 μL 2×NAD⁺基底混合物，反应开始。加入150 μL 1.5 mM 苯甲酰胺反应停止。170uL反应终止液转移到链霉亲和素包被的闪熔镀层上，温育1小时，用微型板块闪烁计数器计数。
细胞实验：^[2]	- 合并 Cell lines: C41细胞 Concentrations: 10 μM 左右 Incubation Time: 0.5小时 Method: 在96孔板上用ABT-888处理C41细胞0.5小时。用1 mM H₂O₂破坏DNA10分钟，PARP被激活。用冰冻的PBS冲洗细胞，然后用预冷的甲醇/丙酮（按7:3比例混合）在−20^oC下固定10 分钟。风干后，用PBS再溶解，然后用溶有5%脱脂奶粉的PBS- Tween封闭液(0.05%)在室温下阻断0.5小时。细胞和PAR抗体按1：50比例在封闭液中室温下温育1小时，然后用PBS-Tween-20冲洗5分钟，然后加入荧光素-5(6)-异硫氰酸酯 (FITC)-联用的二抗和1μg/mL DAPI封闭液中室温下温育1小时。PBS-Tween-20冲洗5分钟后，用荧光微型版计数器分析数据。 (Only for Reference)
动物实验：^[1]	- 合并 Animal Models: 携带NCI-H460, H460, B16F10和9L移植瘤的C57BL/6鼠 Dosages: 25或3.125 mg/kg Administration: 口服处理 (Only for Reference)

参考文献

[4] Kinders RJ, et al, Clin Cancer Res, 2008, 14(21), 6877-6885.

- 合并

溶解度 (25°C)

体外	DMSO	17 mg/mL (69.58 mM)
	Water	Insoluble
	Ethanol	Insoluble
体内	从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 0.5% methylcellulose+0.2% Tween 80	5 mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据 Download Veliparib (ABT-888) SDF

分子量	244.29
化学式	C₁₃H₁₆N₄O
CAS号	912444-00-9
储存条件	3年-20°C 粉状 2年-80°C 溶于溶剂
别名	NSC 737664

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO+ % + % Tween 80+ % ddH₂O

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

质量

浓度

体积

分子量
=

×

×

*在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入输出 )

C1

V1

C2

V2
×

=

×

在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

分子量计算器

通过输入化合物的化学式来计算其分子量：

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×
计算

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-05-17)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03044795	Withdrawn	Drug: Veliparib	Cancer	University Medical Center Groningen\|AbbVie\|Dutch Cancer Society	November 2019	Phase 2
NCT02723864	Active not recruiting	Drug: Veliparib + VX-970 + Cisplatin	Neoplasms	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	August 9 2017	Phase 1
NCT02483104	Completed	Drug: veliparib\|Drug: carboplatin\|Drug: paclitaxel	Ovarian Cancer	AbbVie	July 2015	Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

PARP Signaling Pathway Map

PARP Inhibitors with Unique Features

选择性强的PARP抑制剂

AG-14361 : PARP1-selective, K_i<5 nM.
活性最高的PARP抑制剂

MK-4827 (Niraparib) : PARP1, IC50=3.8 nM; PARP2, IC50=2.1 nM.
用于临床的PARP抑制剂

Iniparib (BSI-201) : Phase III for solid tumors.
最新的PARP抑制剂

BMN 673 : Novel PARP inhibitor with IC50 of 0.58 nM. Also a potent inhibitor of PARP-2, but does not inhibit PARG and highly sensitive to PTEN mutation.

研究领域

产品类型

定制您的化合物库

Veliparib (ABT-888)

客户使用Selleck生产的Veliparib (ABT-888)发表文献182篇：

产品安全说明书

PARP抑制剂选择性比较

生物活性

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

参考文献

溶解度 (25°C)

化学数据 Download Veliparib (ABT-888) SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-05-17)

技术支持

PARP Signaling Pathway Map

PARP Inhibitors with Unique Features

相关PARP产品