ABT-888 (Veliparib) is an orally-available, benzimidazole-based inhibitor of poly(ADP-ribose) polymerase with Ki values of 5.2 and 2.9 nM, for PARP1 and PARP2, respectively. [1] ABT-888 exhibits activity in C41 whole cells at an EC50 of 2 nM [2], and inhibits PAR formation in cells at an EC50 of 4.5 nM. [3]ABT-888 efficiently crosses the blood-brain barrier and has been shown to potentiate DNA-damaging agents such as temozolomide, cisplatin, carboplatin, cyclophosphamide, irinotecan, and radiation. [1, 4] Treatment with temozolomide in the S phase generated higher levels of double-stranded DNA breaks and general higher levels of cytoxicity.
Technical information:
| Chemical Formula: | C13H16N4O | |
| CAS #: | 912444-00-9,912445-05-7 | |
| Molecular Weight: | 244.29 | |
| Purity: | > 98% | |
| Appearance: | White solid | |
| Chemical Name: | (R)-2-(2-methylpyrrolidin-2-yl)-1H-benzo[d]imidazole-4-carboxamide | |
| Solubility: | Up to 75 mM in DMSO | |
| Synonyms: | ABT-888, ABT 888, ABT888, Veliparib |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Palma et al., The PARP inhibitor, ABT-888 potentiates temozolomide: correlation with drug levels and reduction in PARP activity in vivo. Anticancer Res. 2008, 28, 2625-2636. Pubmed ID:19035287 |
| 2. | Penning et al., Discovery of the Poly(ADP-ribose) polymerase (PARP) inhibitor 2-[(R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (ABT-888) for the treatment of cancer. J. Med. Chem. 2009, 52, 514-523. Pubmed ID:19143569 |
| 3. | Liu et al., Potentiation of temozolomide cytotoxicity by poly(ADP)ribose polymerase inhibitor ABT-888 requires a conversion of single-stranded DNA damages to double-stranded DNA breaks. Mol. Cancer Res. 2008, 6, 1621-1629. Pubmed ID:18922977 |
| 4. | Donawho 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, 13(9), 2728-2737. Pubmed ID:19143569 |
Other Information:
Product Specification (pdf) MSDS (pdf) Certificate of Analysis is available upon request.
