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Purity: ≥98%
Veliparib (also known as ABT888; ABT-888) is a novel and potent inhibitor of PARP1 and PARP2 [Poly (ADP-Ribose) Polymerase] with potential anticancer activity. In cell-free assays, it inhibits PARP1/2 with Ki values of 5.2 nM and 2.9 nM, respectively. Abbvie is looking into it as a potential treatment for ovarian and BRCA breast cancer. In addition to its antitumor and chemosensitizing properties, veliparib has no effect on SIRT2. When combined with a range of cytotoxic agents, ABT-888 has shown excellent in vivo efficacy in a broad spectrum of preclinical tumor models. Compared to microsatellite stable (MSS) cell lines (wild-type for both genes), ABT-888 is also active on microsatellite instability (MSI) cell lines carrying mutations in both the MRE11 and RAD50 genes. At therapeutic concentrations, ABT-888 has no antiproliferative effects. Instead, it inhibits PARPs, which prevents DNA repair and increases the cytotoxicity of agents that damage DNA.
| Targets |
PARP-2 ( IC50 = 2.9 nM ); PARP-1 ( IC50 = 5.2 nM ); Autophagy
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| ln Vivo |
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| Enzyme Assay |
Using a commercial assay kit, PARP1 enzyme activity is measured; however, instead of using the PARP1 protein that comes with the kit, cell lysates containing either the wild-type PARP1 or the PARP Y907 mutant are used. Each reaction receives 500 ng of the entire lysate. Veliparib (ABT-888), a PARP inhibitor, has a dosage range of 0.01 to 1,000 μM. A plate reader is used to measure the PARP enzyme activity of both wild-type and mutant samples following their incubation with the substrate[2].
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| Cell Assay |
The Cell Counting Kit-8 (CCK-8) is used to measure the viability of cells. Dojindo's highly water-soluble tetrazolium salt serves as the foundation for this assay. Cells' dehydrogenases reduce WST-8 to produce an orange, water-soluble formazan dye. The number of live cells is directly correlated with the amount of formazan dye produced by cell dehydrogenases. In short, 10,000 cells/well of exponentially growing HaCaT cells are seeded in 96-well plates. The CCK-8 reagent is added 6 or 24 hours after the administration of Veliparib and exposure to sulfur mustard (SM)[3].
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| Animal Protocol |
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| References |
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| Molecular Formula |
C13H16N4O
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| Molecular Weight |
244.29
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| Exact Mass |
244.13
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| Elemental Analysis |
C, 63.91; H, 6.60; N, 22.93; O, 6.55
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| CAS # |
912444-00-9
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| Related CAS # |
912445-05-7 (Veliparib dihydrochloride);912444-00-9
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| Appearance |
White to off-white solid powder
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| SMILES |
C[C@@]1(CCCN1)C2=NC3=C(C=CC=C3N2)C(=O)N
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| InChi Key |
JNAHVYVRKWKWKQ-CYBMUJFWSA-N
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| InChi Code |
InChI=1S/C13H16N4O/c1-13(6-3-7-15-13)12-16-9-5-2-4-8(11(14)18)10(9)17-12/h2,4-5,15H,3,6-7H2,1H3,(H2,14,18)(H,16,17)/t13-/m1/s1
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| Chemical Name |
2-[(2R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide
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| Synonyms |
NSC 737664; NSC737664; NSC-737664; ABT888; ABT-888; ABT 888; Veliparib hydrochloride; Veliparib HCl;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.51 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (8.51 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (8.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 0.5% methylcellulose+0.2% Tween 80: 5mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0935 mL | 20.4675 mL | 40.9350 mL | |
| 5 mM | 0.8187 mL | 4.0935 mL | 8.1870 mL | |
| 10 mM | 0.4093 mL | 2.0467 mL | 4.0935 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03581292 | Active Recruiting |
Drug: Veliparib Drug: Temozolomide |
Glioblastoma (AML) Malignant Glioma |
National Cancer Institute (NCI) |
November 6, 2018 | Phase 2 |
| NCT02163694 | Active Recruiting |
Drug: Veliparib Drug: Veliparib Placebo |
Metastatic Breast Cancer | AbbVie | July 17, 2014 | Phase 3 |
| NCT02595905 | Active Recruiting |
Drug: Veliparib Drug: Cisplatin |
Metastatic Breast Carcinoma Recurrent Breast Carcinoma |
National Cancer Institute (NCI) |
September 15, 2016 | Phase 2 |
| NCT02631733 | Active Recruiting |
Drug: Ferumoxytol Drug: Veliparib |
Malignant Solid Neoplasm | National Cancer Institute (NCI) |
May 31, 2017 | Phase 1 |
| NCT01434316 | Active Recruiting |
Drug: Veliparib Drug: Dinaciclib |
Advanced Malignant Solid Neoplasm | National Cancer Institute (NCI) |
November 1, 2011 | Phase 1 |
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