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United States 

ABT-888

PARP inhibitor
 
ALX-270-444-M001 1 mg 74.00 USD
 
ALX-270-444-M005 5 mg 157.00 USD
 
ALX-270-444-M025 25 mg 422.00 USD
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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 Specification

Alternative Name:2-[(2R)-2-Methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide . dihydrochloride
 
Formula:C13H16N4O . 2HCl
 
MW:244.3 . 73.0
 
CAS:912445-05-7
 
Purity:≥98% (HPLC)
 
Identity:Identity determined by 1H-NMR.
 
Appearance:Colorless to white crystalline solid.
 
Solubility:Soluble in water or DMSO.
 
Shipping:Ambient
 
Long Term Storage:-20°C
 
270-444
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Product Literature References

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;
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;

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