Veliparib (ABT-888)
别名: NSC 737664 中文名称：维利帕尼
Veliparib (ABT-888, NSC 737664)是一种有效的PARP1和PARP2抑制剂，无细胞试验中Ki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。
Veliparib (ABT-888) Chemical Structure
CAS: 912444-00-9
客户使用Selleck的Veliparib (ABT-888)发表文献226篇
产品质控
Veliparib (ABT-888)相关产品
相关信号通路图
PARP抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| LoVo | Cytotoxicity assay | 0.4 uM | 5 days | Potentiation of temozolomide-induced cytotoxicity in human LoVo cells assessed as temozolomide GI50 at 0.4 uM after 5 days by Celltiter-Glo assay, GI50 = 6.203 μM. | 26652717 |
| FaDu | Cytotoxic Assay | 10 μM | 24 h | Reduces the cell viability | 21912620 |
| UM-SCC1 | Cytotoxic Assay | 10 μM | 24 h | Reduces the cell viability | 21912620 |
| HCT-116 | Kinase Assay | 0.5 μM | 24 h | PARP activity decreases | 23054213 |
| ML-1 | Apoptotic Assay | 2.5 μM | 24 h | Synergistically enhances TRAIL-induced apoptosis in ML-1 cells | 24895135 |
| PC-3 | Growth Inhibition Assay | 10 μM | Induces a significant inhibition in colony formation | 21571912 | |
| VC8 | Cytotoxicity assay | 3 days | Cytotoxicity against Chinese hamster VC8 cells harboring BRCA2 deficient after 3 days by CCK8 assay, CC50 = 2.344 μM. | 29335205 | |
| LoVo | Function assay | 30 mins | Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay, EC50 = 0.00594 μM. | 26652717 | |
| LoVo | Function assay | 30 mins | Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay, EC50 = 0.00594 μM. | 26652717 | |
| LoVo | Function assay | 30 mins | Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay, EC50 = 0.00594 μM. | 26652717 | |
| DT40 | Cytotoxic Assay | 72 h | Cytotoxicity against chicken BRCA2-deficient DT40 cells | 24922587 | |
| Capan1 | Growth Inhibition Assay | 72 h | Antiproliferative activity against BRCA2 gene mutated human Capan1 cells with IC50 of 39.7 μM | 24398383 | |
| Jurkat | Kinase Assay | 96 h | Inhibition of PARP1 assessed as reduction of cell viability with EC50 of 3 μM | 23850199 | |
| C41 | Kinase Assay | 30 min | Inhibition of PARP1 with EC50 of 0.002 μM | 19888760 | |
| SK-MEL-24 | Growth Inhibition Assay | IC50=7.81924 μM | SANGER | ||
| HCC2218 | Growth Inhibition Assay | IC50=7.79704 μM | SANGER | ||
| COLO-680 | Growth Inhibition Assay | IC50=6.21406 μM | SANGER | ||
| HCC1806 | Growth Inhibition Assay | IC50=5.75173 μM | SANGER | ||
| BV-173 | Growth Inhibition Assay | IC50=5.45409 μM | SANGER | ||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=3.12841 μM | SANGER | ||
| EoL-1-cell | Growth Inhibition Assay | IC50=1.0798 μM | SANGER | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SK-N-SH cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| C41 | Function assay | Inhibition of PARP1 in human C41 cells, EC50 = 0.002 μM. | 19143569 | ||
| NCI-H720 | Growth Inhibition Assay | IC50=8.43603 μM | SANGER | ||
| KASUMI-1 | Growth Inhibition Assay | IC50=8.89266 μM | SANGER | ||
| HAL-01 | Growth Inhibition Assay | IC50=9.8862 μM | SANGER | ||
| CAL-33 | Growth Inhibition Assay | IC50=10.434 μM | SANGER | ||
| SK-MEL-1 | Growth Inhibition Assay | IC50=12.4663 μM | SANGER | ||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=12.4752 μM | SANGER | ||
| KY821 | Growth Inhibition Assay | IC50=12.485 μM | SANGER | ||
| HEC-1 | Growth Inhibition Assay | IC50=12.9196 μM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=13.166 μM | SANGER | ||
| MN-60 | Growth Inhibition Assay | IC50=13.5389 μM | SANGER | ||
| DU-145 | Growth Inhibition Assay | IC50=13.9053 μM | SANGER | ||
| EW-3 | Growth Inhibition Assay | IC50=14.5565 μM | SANGER | ||
| OS-RC-2 | Growth Inhibition Assay | IC50=15.9589 μM | SANGER | ||
| RPMI-8226 | Growth Inhibition Assay | IC50=16.2042 μM | SANGER | ||
| ChaGo-K-1 | Growth Inhibition Assay | IC50=16.5325 μM | SANGER | ||
| DEL | Growth Inhibition Assay | IC50=16.6717 μM | SANGER | ||
| GP5d | Growth Inhibition Assay | IC50=17.053 μM | SANGER | ||
| COLO-668 | Growth Inhibition Assay | IC50=17.6294 μM | SANGER | ||
| H9 | Growth Inhibition Assay | IC50=18.2833 μM | SANGER | ||
| NKM-1 | Growth Inhibition Assay | IC50=18.5119 μM | SANGER | ||
| KYSE-150 | Growth Inhibition Assay | IC50=18.9986 μM | SANGER | ||
| Daoy | Growth Inhibition Assay | IC50=19.5649 μM | SANGER | ||
| ECC10 | Growth Inhibition Assay | IC50=20.7455 μM | SANGER | ||
| A388 | Growth Inhibition Assay | IC50=21.9091 μM | SANGER | ||
| MHH-NB-11 | Growth Inhibition Assay | IC50=23.1363 μM | SANGER | ||
| HCC1937 | Growth Inhibition Assay | IC50=24.746 μM | SANGER | ||
| TGBC11TKB | Growth Inhibition Assay | IC50=25.6863 μM | SANGER | ||
| CTV-1 | Growth Inhibition Assay | IC50=25.8969 μM | SANGER | ||
| NCI-H2029 | Growth Inhibition Assay | IC50=26.4238 μM | SANGER | ||
| HLE | Growth Inhibition Assay | IC50=27.054 μM | SANGER | ||
| NCI-H1693 | Growth Inhibition Assay | IC50=27.2898 μM | SANGER | ||
| HCC70 | Growth Inhibition Assay | IC50=27.7246 μM | SANGER | ||
| BEN | Growth Inhibition Assay | IC50=27.9566 μM | SANGER | ||
| LB771 | Growth Inhibition Assay | IC50=28.8373 μM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=29.0235 μM | SANGER | ||
| LU-139 | Growth Inhibition Assay | IC50=29.3748 μM | SANGER | ||
| EW-13 | Growth Inhibition Assay | IC50=29.3814 μM | SANGER | ||
| MOLT-13 | Growth Inhibition Assay | IC50=29.3814 μM | SANGER | ||
| L-363 | Growth Inhibition Assay | IC50=29.4798 μM | SANGER | ||
| EM-2 | Growth Inhibition Assay | IC50=29.4901 μM | SANGER | ||
| RS4-11 | Growth Inhibition Assay | IC50=30.4241 μM | SANGER | ||
| A2780 | Growth Inhibition Assay | IC50=30.7457 μM | SANGER | ||
| KU812 | Growth Inhibition Assay | IC50=32.3642 μM | SANGER | ||
| COLO-684 | Growth Inhibition Assay | IC50=33.3599 μM | SANGER | ||
| MFE-280 | Growth Inhibition Assay | IC50=33.3889 μM | SANGER | ||
| KG-1 | Growth Inhibition Assay | IC50=33.6001 μM | SANGER | ||
| JVM-3 | Growth Inhibition Assay | IC50=35.5868 μM | SANGER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=35.8499 μM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=36.7345 μM | SANGER | ||
| MOLT-16 | Growth Inhibition Assay | IC50=36.952 μM | SANGER | ||
| H4 | Growth Inhibition Assay | IC50=37.567 μM | SANGER | ||
| T47D | Growth Inhibition Assay | IC50=37.7018 μM | SANGER | ||
| CAL-54 | Growth Inhibition Assay | IC50=37.966 μM | SANGER | ||
| SW982 | Growth Inhibition Assay | IC50=38.0998 μM | SANGER | ||
| IGROV-1 | Growth Inhibition Assay | IC50=39.3304 μM | SANGER | ||
| NB14 | Growth Inhibition Assay | IC50=40.7031 μM | SANGER | ||
| HCC1187 | Growth Inhibition Assay | IC50=41.2771 μM | SANGER | ||
| SBC-1 | Growth Inhibition Assay | IC50=41.3063 μM | SANGER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=41.4818 μM | SANGER | ||
| MOLT-4 | Growth Inhibition Assay | IC50=42.2538 μM | SANGER | ||
| JVM-2 | Growth Inhibition Assay | IC50=42.9207 μM | SANGER | ||
| A4-Fuk | Growth Inhibition Assay | IC50=43.5691 μM | SANGER | ||
| MDA-MB-361 | Growth Inhibition Assay | IC50=43.8414 μM | SANGER | ||
| BALL-1 | Growth Inhibition Assay | IC50=43.9532 μM | SANGER | ||
| T98G | Growth Inhibition Assay | IC50=44.8517 μM | SANGER | ||
| Mo-T | Growth Inhibition Assay | IC50=45.6389 μM | SANGER | ||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=45.7585 μM | SANGER | ||
| ALL-PO | Growth Inhibition Assay | IC50=47.3791 μM | SANGER | ||
| NCI-H510A | Growth Inhibition Assay | IC50=47.9034 μM | SANGER | ||
| ML-2 | Growth Inhibition Assay | IC50=49.7856 μM | SANGER | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Veliparib (ABT-888, NSC 737664)是一种有效的PARP1和PARP2抑制剂，无细胞试验中Ki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。 | ||||
|---|---|---|---|---|---|
| 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 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | ABT-888有效抑制PARP，作用于PARP-1和PARP-2时Ki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] |
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|---|---|---|---|---|
| 激酶实验 | 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 | 细胞系 | C41细胞 | ||
| 浓度 | 10 μM 左右 | |||
| 孵育时间 | 0.5小时 | |||
| 方法 | 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−20oC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。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-STAT3 / STAT3 / p-AKT(S473) / p-AKT(T308) / p-ERK / p-p38 |
|
22678161 | |
| Immunofluorescence | HuR BRCA1 |
|
28687616 | |
| Growth inhibition assay | Cell viability (TNBC cell lines) Cell viability (melanoma cells) |
|
27880910 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 |
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] |
|
|---|---|---|
| 动物实验 | 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 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03044795 | Withdrawn | Cancer |
University Medical Center Groningen|AbbVie|Dutch Cancer Society |
November 2019 | Phase 2 |
| NCT02723864 | Completed | Neoplasms |
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
August 9 2017 | Phase 1 |
| NCT02483104 | Completed | Ovarian Cancer |
AbbVie |
July 2015 | Phase 1 |
化学信息&溶解度
| 分子量 | 244.29 | 分子式 | C13H16N4O |
| CAS号 | 912444-00-9 | SDF | Download Veliparib (ABT-888) SDF |
| Smiles | CC1(CCCN1)C2=NC3=C(C=CC=C3N2)C(=O)N | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 49 mg/mL ( (200.58 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
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）
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）
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。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，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。
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