Potent inhibitor of PARP-1 and PARP-2 (potency ≤5nM in vitro). Does not inhibit other NAD-binding enzymes. Has minimal CYP450 inhibition and induction. Shows broad spectrum of chemo- and radiopotentiation. Is toxic to both oxic and hypoxic cells. Enantiomeric purity ≥97% suitable for in vivo studies. Does not show inherent cytotoxicity and shows no single agent activity in tumor models. Has excellent bioavailability and good blood-brain permeation. Increases tumor growth delay resulting from radiation and DNA-damaging agents.
Product Details
| Alternative Name: | 2-[(2R)-2-Methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide . dihydrochloride |
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| Formula: | C13H16N4O . 2HCl |
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| MW: | 244.3 . 73.0 |
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| CAS: | 912445-05-7 |
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| Purity: | ≥98% (HPLC) |
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| Identity: | Identity determined by 1H-NMR. |
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| Appearance: | Colorless to white crystalline solid. |
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| Solubility: | Soluble in water or DMSO. |
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| Shipping: | Ambient |
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| Long Term Storage: | -20°C |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Decreased expression of the translation factor eIF3e induces senescence in breast cancer cells via suppression of PARP1 and activation of mTORC1: C. Morris, et al.; Oncotarget
12, 649 (2021),
Abstract;
Full Text
Analysis of PARP inhibitor toxicity by multidimensional fluorescence microscopy reveals mechanisms of sensitivity and resistance: J. Michelena, et al.; Nat. Commun.
9, 2678 (2018),
Abstract;
Full Text
ABT-888 and Quinacrine induced apoptosis in metastatic breast cancer stem cells by inhibiting base excision repair via Adenomatous polyposis coli: S. Siddharth, et al. ; DNA Repair (Amst.)
45, 44 (2016),
Application(s): Cell culture,
Abstract;
Common and unique genetic interactions of the poly(ADP-ribose) polymerases PARP1 and PARP2 with DNA double-strand break repair pathways: R. Ghosh, et al.; DNA Repair (Amst.)
45, 56 (2016),
Application(s): Genomic instability in metaphase spreads of wt and H2afx-/- activated B cells,
Abstract;
Disrupted ADP-ribose metabolism with nuclear Poly (ADP-ribose) accumulation leads to different cell death pathways in presence of hydrogen peroxide in procyclic Trypanosoma brucei: M. Schlesinger, et al.; Parasit. Vectors
9, 173 (2016),
Application(s): Potency of inhibitors,
Abstract;
Full Text
p53 coordinates base excision repair to prevent genomic instability: M. Poletto, et al.; Nucleic Acids Res.
44, 3165 (2016),
Application(s): Cell culture,
Abstract;
Full Text
p53 induces formation of NEAT1 lncRNA-containing paraspeckles that modulate replication stress response and chemosensitivity: C. Adriaens, et al.; Nat. Med.
22, 861 (2016),
Application(s): Long-term growth assays,
Abstract;
Full Text
Increased in vitro and in vivo sensitivity of BRCA2-associated pancreatic cancer to the poly(ADP-ribose) polymerase-1/2 inhibitor BMN 673: A.Z. Andrei, et al.; Cancer Lett.
364, 8 (2015),
Application(s): Cell Culture,
Abstract;
53BP1 mediates the fusion of mammalian telomeres rendered dysfunctional by DNA-PKcs loss or inhibition: I. Rybanska-Spaeder, et al.; PLoS One
9, e10873 (2014),
Abstract;
Full Text
Role for DNA damage signaling in pulmonary arterial hypertension: J. Meloche, et al.; Circulation
129, 786 (2014),
Abstract;
ATR inhibition broadly sensitizes ovarian cancer cells to chemotherapy independent of BRCA status: C.J. Huntoon, et al.; Cancer Res.
73, 3683 (2013),
Abstract;
Evaluation of poly (ADP-ribose) polymerase inhibitor ABT-888 combined with radiotherapy and temozolomide in glioblastoma: L. Barazzuol, et al.; Radiat. Oncol.
8, 65 (2013),
Abstract;
Full Text
Inhibition of PARP1 by small interfering RNA enhances docetaxel activity against human prostate cancer PC3 cells: W. Wu, et al.; BBRC
442, 127 (2013),
Abstract;
Inhibition of poly(ADP-ribose) polymerase-1 or poly(ADP-ribose) glycohydrolase individually, but not in combination, leads to improved chemotherapeutic efficacy in HeLa cells: X. Feng, et al.; Int. J. Onc.
42, 749 (2013),
Abstract;
Full Text
The Forkhead Box M1 protein regulates BRIP1 expression and DNA damage repair in epirubicin treatment: L.J. Monteiro, et al.; Oncogene
32, 4634 (2013),
Abstract;
Disposition and Drug-Drug Interaction Potential of Veliparib (ABT-888), a Novel and Potent Inhibitor of Poly(ADP-ribose) Polymerase: X. Li, et al.; Drug Metab. Dispos.
39, 1161 (2011),
Abstract;
Nonhomologous end joining drives poly(ADP-ribose) polymerase (PARP) inhibitor lethality in homologous recombination-deficient cells: A.G. Patel, et al.; PNAS
108, 3406 (2011),
Abstract;
Inhibition of poly(ADP-ribose) polymerase down-regulates BRCA1 and RAD51 in a pathway mediated by E2F4 and p130: D.C. Hegan, et al.; PNAS
107, 2201 (2010),
Abstract;
Full Text
Plasma and cerebrospinal fluid pharmacokinetics of ABT-888 after oral administration in non-human primates: J.A. Muscal, et al.; Cancer Chemother. Pharmacol.
65, 419 (2010),
Abstract;
PTEN loss compromises homologous recombination repair in astrocytes: implications for glioblastoma therapy with temozolomide or poly(ADP-ribose) polymerase inhibitors: B. McEllin, et al.; Cancer Res.
70, 5457 (2010),
Abstract;
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: T.D. Penning, et al.; J. Med. Chem.
52, 514 (2009),
Abstract;
A novel poly(ADP-ribose) polymerase inhibitor, ABT-888, radiosensitizes malignant human cell lines under hypoxia: S.K. Liu, et al.; Radiother. Oncol.
88, 258 (2008),
Abstract;
ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models: C.K. Donawho, et al.; Clin. Cancer Res.
13, 2728 (2007),
Abstract;
Inhibition of poly(ADP-ribose) polymerase enhances cell death and improves tumor growth delay in irradiated lung cancer models: J.M. Albert, et al.; Clin. Cancer Res.
13, 3033 (2007),
Abstract;
