Veliparib (ABT-888)

Catalog No.S1004

Veliparib (ABT-888) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Phase 3.

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Veliparib (ABT-888) Chemical Structure

Veliparib (ABT-888) Chemical Structure
Molecular Weight: 244.29

Validation & Quality Control

Cited by 37 publications:

9 customer reviews :

Quality Control & MSDS

Related Compound Libraries

Veliparib (ABT-888) is available in the following compound libraries:

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  • Newest PARP Inhibitor

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Product Information

  • Compare PARP Inhibitors
    Compare PARP Products
  • Research Area
  • Veliparib (ABT-888) Mechanism
  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

Description Veliparib (ABT-888) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Phase 3.
Targets PARP2 [1]
(Cell-free assay)
PARP1 [1]
(Cell-free assay)
IC50 2.9 nM(Ki) 5.2 nM(Ki)
In vitro ABT-888 is inactive to SIRT2 (>5 μM). [1] ABT-888 inhibits the PARP activity with EC50 of 2 nM in C41 cells. [2] ABT-888 could decrease the PAR levels in both irradiated and nonirradiated H460 cells. ABT-888 also reduces clonogenic survival and inhibits DNA repair by PARP-1 inhibition in H460 cells. ABT-888 increases apoptosis and autophagy in H460 cells when combination with radiation. [3] ABT-888 also inhibits PARP activity in H1299, DU145 and 22RV1 cells and the inhibition is independent of p53 function. ABT-888 (10 μM) suppresses the surviving fraction (SF) by 43% in the clonogenic H1299 cells. ABT-888 shows effective radiosensitivity in oxic H1299 cells. Furthermore, ABT-888 could attenuate the SF of hypoxic-irradiated cells including H1299, DU145 and 22RV1. [4]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
C41MYXLbY5ie2ViQYPzZZk>NYnZdVdQOzBibXnuM4XxWGlvcGmkaYTpc44hd2ZiUFHSVFEhf2m2aDDFR|UxKG:oIECuNFAzKM7:TR?=NEXrdYgyQTh6OEe2NC=>
JurkatMXzLbY5ie2ViQYPzZZk>MmLzPVYhcA>?M{O3WWROW09?NFnhUopKdmirYnn0bY9vKG:oIGDBVnAyKGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBk\WyuII\pZYJqdGm2eTD3bZRpKEWFNUCgc4YhOyEQvF2=NHXRWIgzOzh3MEG5PS=>
Capan1M1S2bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M{m1PFczKGh?M3\MVGROW09?NEHUPXZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGJTS0F{IHflcoUhdXW2YYTl[EBpfW2jbjDDZZBidjFiY3XscJMhf2m2aDDJR|UxKG:oIEO5Mlch|ryPNIDG[YkzPDN7OEO4Ny=>
DT40NEP0[mFEgXSxdH;4bYMhSXO|YYm=NUPoVVhEPzJiaB?=M3nXV2ROW09?NELFboJEgXSxdH;4bYNqfHliYXfhbY5{fCClaHnjb4VvKEKUQ1GyMYRm\mmlaXXueEBFXDRyIHPlcIx{MUeyOFkzOjV6Nx?=
ML-1NX7xTmpPSXCxcITveIlkKEG|c3H5MmmyNk42KM7:TR?=M1rtUVI1KGh?MmT3SG1UVw>?NIDvXoFUgW6ncnfpd5Rq[2GubImg[Y5p[W6lZYOgWHJCUUxvaX7keYNm\CCjcH;weI9{cXNiaX6gUWwuOSClZXzsdy=>NFfxT3MzPDh7NUGzOS=>
HCT-116Ml3IT4lv[XOnIFHzd4F6NWfFfYk3OC53IN88US=>NX3HNpV7OjRiaB?=MWDQRXJRKGGldHn2bZR6KGSnY4LlZZNmew>?MofCNlMxPTR{MUO=
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... Click to View More Cell Line Experimental Data

In vivo The oral bioavailability of ABT-888 is 56%-92% in mice, Sprague-Dawley rats, beagle dogs, and cynomolgus monkeys after oral administration. [1] ABT-888 (25 mg/kg i.p.) could improve tumor growth delay in a NCI-H460 xenograft model with well tolerated. Combination with radiation, ABT-888 decreases the tumor vessel formation. [3] ABT-888 reduces intratumor PAR levels by more than 95% at a dose of 3 and 12.5 mg/kg in A375 and Colo829 xenograft models and the suppression could be maintained over time. [4]
Features Increases the efficacy of common cancer therapies such as radiation and alkylating agents.

Protocol(Only for Reference)

Kinase Assay:

[1]

In vitro PARP assays PARP assays are conducted in a buffer containing 50 mM Tris (pH 8.0), 1 mM DTT, 1.5 μM [3H]NAD+ (1.6 μCi/mmol), 200 nM biotinylated histone H1, 200 nM slDNA, and 1 nM PARP-1 or 4 nM PARP-2 enzyme. Reactions are terminated with 1.5 mM benzamide, transferred to streptavidin Flash plates, and counted using a TopCount microplate scintillation counter.

Animal Study:

[1]

Animal Models NCI-H460, H460, B16F10 and 9L xenografts in C57BL/6 mice
Formulation Formulated in solution containing 0.9% NaCl adjusted to pH 4.0
Dosages ~25 mg/kg
Administration Orally administered

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Donawho CK, et al, Clin Cancer Res, 2007, 13 (9), 2728-2737.

[2] Penning TD, et al, J Med Chem, 2009, 52(2), 514-523.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-06-25)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02595905 Not yet recruiting BRCA1 Mutation Carrier|BRCA2 Mutation Carrier|Estrogen Receptor Negative|HER2/Neu Negative|Progesterone Receptor Negative|Stage IV Breast Cancer|Tr  ...more BRCA1 Mutation Carrier|BRCA2 Mutation Carrier|Estrogen Receptor Negative|HER2/Neu Negative|Progesterone Receptor Negative|Stage IV Breast Cancer|Triple-Negative Breast Carcinoma National Cancer Institute (NCI) July 2016 Phase 2
NCT02631733 Not yet recruiting Estrogen Receptor Negative|HER2/Neu Negative|Neuroendocrine Neoplasm|Progesterone Receptor Negative|Stage IIB Cervical Cancer|Stage IIIA Cervical C  ...more Estrogen Receptor Negative|HER2/Neu Negative|Neuroendocrine Neoplasm|Progesterone Receptor Negative|Stage IIB Cervical Cancer|Stage IIIA Cervical Cancer|Stage IIIB Cervical Cancer|Stage IIIB Non-Small Cell Lung Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer|Stage IV Cervical Cancer|Stage IV Gastric Cancer|Stage IV Non-Small Cell Lung Cancer|Stage IV Ovarian Cancer|Stage IV Small Cell Lung Carcinoma|Triple-Negative Breast Carcinoma National Cancer Institute (NCI) May 2016 Phase 1
NCT02723864 Recruiting Neoplasms National Cancer Institute (NCI)|National Institutes of He  ...more National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) March 2016 Phase 1
NCT02483104 Active, not recruiting Ovarian Cancer AbbVie July 2015 Phase 1
NCT02470585 Recruiting Ovarian Cancer|Ovarian Neoplasm AbbVie|Gynecologic Oncology Group July 2015 Phase 3

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Chemical Information

Download Veliparib (ABT-888) SDF
Molecular Weight (MW) 244.29
Formula

C13H16N4O

CAS No. 912444-00-9
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms NSC 737664
Solubility (25°C) * In vitro DMSO 17 mg/mL (69.58 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 0.5% methylcellulose+0.2% Tween 80 5 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name (R)-2-(2-methylpyrrolidin-2-yl)-1H-benzo[d]imidazole-4-carboxamide

Customer Product Validation(9)


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Source Cancer Research, 2011, 71: 4944-4954. Veliparib (ABT-888) purchased from Selleck
Method Clonogenic Assays
Cell Lines OVCAR-8 cells
Concentrations 3 µmol/L
Incubation Time 8 d
Results A: Both PARP inhibitors markedly increased killing when cells were co-exposed to FdUrd and the PARP inhibitor for 24 h (Fig. A), followed by continuous treatment with the PARP inhibitor. B: The concentration of FdUrd that inhibited proliferation by 50% (IC50) was reduced when cells were continuously exposed to ABT-888 and ABT-888 also potentiated the effects of FdUrd in OVCAR-8. C: The data indicated strong synergistic killing over a wide range of concentrations.

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Source Cancer Research, 2011, 71: 4944-4954. Veliparib (ABT-888) purchased from Selleck
Method Clonogenic Assays
Cell Lines OVCAR-8 cells
Concentrations 3 µmol/L
Incubation Time 8 d
Results :We compared a series of FdUrd and ABT-888 exposure schemes (Fig. C). Modestly increased cytotoxicity was observed when OVCAR-8 cells were exposed to FdUrd and ABT-888 simultaneously for 24 h (Sequence II), compared to FdUrd alone (Sequence I)(Fig. D). Similarly, exposure to FdUrd alone for 24 h followed by continuous incubation with ABT-888 modestly increased cytotoxicity over FdUrd alone (Sequence III). In contrast, the most robust killing was seen with Sequences IV and V, in which cells were simultaneously exposed to FdUrd and ABT-888, followed by continuous ABT-888 treatment after FdUrd removal.

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Source Nucl Med Commun 2011 32, 1046-1051. Veliparib (ABT-888) purchased from Selleck
Method Laser confocal microscopy/fluorescent H2AX Antibody Staining
Cell Lines Epstein–Barr virus-infected Raji lymphocyte tumor cells
Concentrations 500 nM
Incubation Time 2 h
Results The Fluor-647 anti-H2A.X-phosphorylated (Ser139) antibody stained significantly more double-stranded breaks in cells treated with ABT-888 and AZD-2281 compared with controls at 8 and 12 Gy (P<0.05).

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Source Nucl Med Commun 2011 32(11), 1046-51. Veliparib (ABT-888) purchased from Selleck
Method Cell growth assay
Cell Lines human Burkitt lymphoma cells
Concentrations 500 nmol/l
Incubation Time 0-5 d
Results A volume of 500 nmol/l ABT-888 and AZD-2281 showed a moderate intrinsc effect on cell proliferation on days 3–5 (Fig. a). ABT-888 and AZD-2281 showed a significant ( P < 0.05) reduction in lymphoma cell growth on days 2–5 (Fig. b–d).

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Source Nucl Med Commun 2011 32(11), 1046-51. Veliparib (ABT-888) purchased from Selleck
Method PARP activity assay
Cell Lines Raji lymphocyte tumor cells
Concentrations 500 nmol/l
Incubation Time 24 h
Results

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Source Dr.Zhang of Tianjin Medical University. Veliparib (ABT-888) purchased from Selleck
Method Western blot
Cell Lines T47D breast cancer cells
Concentrations 0-5 μM
Incubation Time
Results

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Source David Schrmann from University of Base. Veliparib (ABT-888) purchased from Selleck
Method Kruskal-Wallis and the post-hoc Dunn’s Multiple Comparison tests, immuno-staining
Cell Lines Primary human lung fibroblast cells (MRC-5)
Concentrations 1-100 nM
Incubation Time 2 h
Results

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Source Dr. Steve Reuland from University of Colorado Denver. Veliparib (ABT-888) purchased from Selleck
Method MTS assay
Cell Lines 451 Lu cells
Concentrations 0-400 μM
Incubation Time 120 h
Results Treatment with 25 µM ABT-888 greatly increased sensitivity to temozolomide compared to cells without ABT-888 treatment as measured by MTS assay.

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Source Dr. Xiangbing Meng of University of Iowa. Veliparib (ABT-888) purchased from Selleck
Method WST-1 method
Cell Lines Hec50/Ishikawa/SKOV3/Caov3/PA-1 cell line
Concentrations 0-12000 nM
Incubation Time 3 d
Results ABT-888 decreased the viability of the endometrial cancer cell line Hec50 and Ishikawa and ovarian cancer cell line SKOV3,Caov3 and PA-1 in a dose-dependent manner.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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