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912444-00-9,MFCD16661059
Catalog No.:AA0039I5

912444-00-9 | Veliparib

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1mg
98%
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$7.00   $5.00
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5mg
98%
in stock  
$12.00   $8.00
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10mg
98%
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$15.00   $11.00
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25mg
98%
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$36.00   $25.00
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250mg
98%
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$99.00   $69.00
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1g
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$236.00   $165.00
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  • Technical Information
  • Properties
  • Literature
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  • Technical Information
  • Properties
  • Literature
Technical Information
Catalog Number:
AA0039I5
Chemical Name:
Veliparib
CAS Number:
912444-00-9
Molecular Formula:
C13H16N4O
Molecular Weight:
244.2923
MDL Number:
MFCD16661059
SMILES:
NC(=O)c1cccc2c1[nH]c(n2)[C@@]1(C)CCCN1
NSC Number:
737664
Properties
Computed Properties
 
Complexity:
348  
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
1  
Heavy Atom Count:
18  
Hydrogen Bond Acceptor Count:
3  
Hydrogen Bond Donor Count:
3  
Rotatable Bond Count:
2  
XLogP3:
0.5  

Literature

Title: Analyzing structure-function relationships of artificial and cancer-associated PARP1 variants by reconstituting TALEN-generated HeLa PARP1 knock-out cells.

Journal: Nucleic acids research 20161201

Title: CDK12 Inhibition Reverses De Novo and Acquired PARP Inhibitor Resistance in BRCA Wild-Type and Mutated Models of Triple-Negative Breast Cancer.

Journal: Cell reports 20161122

Title: Adaptive Randomization of Veliparib-Carboplatin Treatment in Breast Cancer.

Journal: The New England journal of medicine 20160707

Title: Sulfur and nitrogen mustards induce characteristic poly(ADP-ribosyl)ation responses in HaCaT keratinocytes with distinctive cellular consequences.

Journal: Toxicology letters 20160226

Title: Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.

Journal: Journal of medicinal chemistry 20150910

Title: Mitochondrial reactive oxygen species are scavenged by Cockayne syndrome B protein in human fibroblasts without nuclear DNA damage.

Journal: Proceedings of the National Academy of Sciences of the United States of America 20140916

Title: Pharmacological Inhibition of poly(ADP-ribose) polymerases improves fitness and mitochondrial function in skeletal muscle.

Journal: Cell metabolism 20140603

Title: Identification of potent Yes1 kinase inhibitors using a library screening approach.

Journal: Bioorganic & medicinal chemistry letters 20130801

Title: Identification of DNA repair pathways that affect the survival of ovarian cancer cells treated with a poly(ADP-ribose) polymerase inhibitor in a novel drug combination.

Journal: Molecular pharmacology 20121001

Title: Poly(ADP-ribose) polymerase 1 modulates the lethality of CHK1 inhibitors in mammary tumors.

Journal: Molecular pharmacology 20120801

Title: Radiation-inducible immunotherapy for cancer: senescent tumor cells as a cancer vaccine.

Journal: Molecular therapy : the journal of the American Society of Gene Therapy 20120501

Title: Poly(ADP-ribose) polymerase 1 inhibition improves coronary arteriole function in type 2 diabetes mellitus.

Journal: Hypertension (Dallas, Tex. : 1979) 20120501

Title: Failure of iniparib to inhibit poly(ADP-Ribose) polymerase in vitro.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20120315

Title: A phase I study of veliparib in combination with metronomic cyclophosphamide in adults with refractory solid tumors and lymphomas.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20120315

Title: The impact of cyclin-dependent kinase 5 depletion on poly(ADP-ribose) polymerase activity and responses to radiation.

Journal: Cellular and molecular life sciences : CMLS 20120301

Title: Enhanced killing of cancer cells by poly(ADP-ribose) polymerase inhibitors and topoisomerase I inhibitors reflects poisoning of both enzymes.

Journal: The Journal of biological chemistry 20120203

Title: Iniparib nonselectively modifies cysteine-containing proteins in tumor cells and is not a bona fide PARP inhibitor.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20120115

Title: Novel binding mode of a potent and selective tankyrase inhibitor.

Journal: PloS one 20120101

Title: Synthetic lethal interactions between EGFR and PARP inhibition in human triple negative breast cancer cells.

Journal: PloS one 20120101

Title: Bortezomib-induced 'BRCAness' sensitizes multiple myeloma cells to PARP inhibitors.

Journal: Blood 20111208

Title: Poly(ADP-ribose) polymerase inhibition enhances p53-dependent and -independent DNA damage responses induced by DNA damaging agent.

Journal: Cell cycle (Georgetown, Tex.) 20111201

Title: Anti-estrogen resistance in breast cancer is induced by the tumor microenvironment and can be overcome by inhibiting mitochondrial function in epithelial cancer cells.

Journal: Cancer biology & therapy 20111115

Title: Veliparib plus temozolomide in metastatic melanoma trends toward increased PFS but results are not statistically significant.

Journal: Oncology (Williston Park, N.Y.) 20111115

Title: Poly(ADP-ribose) polymerase inhibitors combined with external beam and radioimmunotherapy to treat aggressive lymphoma.

Journal: Nuclear medicine communications 20111101

Title: Response of subtype-specific human breast cancer-derived cells to poly(ADP-ribose) polymerase and checkpoint kinase 1 inhibition.

Journal: Cancer science 20111001

Title: Phase I study of PARP inhibitor ABT-888 in combination with topotecan in adults with refractory solid tumors and lymphomas.

Journal: Cancer research 20110901

Title: Poly(ADP-Ribose) polymerase inhibition synergizes with 5-fluorodeoxyuridine but not 5-fluorouracil in ovarian cancer cells.

Journal: Cancer research 20110715

Title: Disposition and drug-drug interaction potential of veliparib (ABT-888), a novel and potent inhibitor of poly(ADP-ribose) polymerase.

Journal: Drug metabolism and disposition: the biological fate of chemicals 20110701

Title: Response of human prostate cancer cells and tumors to combining PARP inhibition with ionizing radiation.

Journal: Molecular cancer therapeutics 20110701

Title: Identification of human triple-negative breast cancer subtypes and preclinical models for selection of targeted therapies.

Journal: The Journal of clinical investigation 20110701

Title: PARP inhibitors: its role in treatment of cancer.

Journal: Chinese journal of cancer 20110701

Title: The poly(ADP-Ribose) polymerase inhibitor ABT-888 reduces radiation-induced nuclear EGFR and augments head and neck tumor response to radiotherapy.

Journal: Radiotherapy and oncology : journal of the European Society for Therapeutic Radiology and Oncology 20110601

Title: Poly(ADP-ribose) polymerase and XPF-ERCC1 participate in distinct pathways for the repair of topoisomerase I-induced DNA damage in mammalian cells.

Journal: Nucleic acids research 20110501

Title: N-methylpurine DNA glycosylase and DNA polymerase beta modulate BER inhibitor potentiation of glioma cells to temozolomide.

Journal: Neuro-oncology 20110501

Title: 5-Benzamidoisoquinolin-1-ones and 5-(ω-carboxyalkyl)isoquinolin-1-ones as isoform-selective inhibitors of poly(ADP-ribose) polymerase 2 (PARP-2).

Journal: Journal of medicinal chemistry 20110414

Title: MRE11 deficiency increases sensitivity to poly(ADP-ribose) polymerase inhibition in microsatellite unstable colorectal cancers.

Journal: Cancer research 20110401

Title: PARP inhibitors in oncology: a new synthetic lethal approach to cancer therapy.

Journal: Acta clinica Belgica 20110101

Title: Cetuximab augments cytotoxicity with poly (adp-ribose) polymerase inhibition in head and neck cancer.

Journal: PloS one 20110101

Title: Modeling pharmacodynamic response to the poly(ADP-Ribose) polymerase inhibitor ABT-888 in human peripheral blood mononuclear cells.

Journal: PloS one 20110101

Title: Cooperation of breast cancer proteins PALB2 and piccolo BRCA2 in stimulating homologous recombination.

Journal: Nature structural & molecular biology 20101001

Title: Poly(ADP-ribose) polymerase inhibitor induces accelerated senescence in irradiated breast cancer cells and tumors.

Journal: Cancer research 20100801

Title: PTEN loss compromises homologous recombination repair in astrocytes: implications for glioblastoma therapy with temozolomide or poly(ADP-ribose) polymerase inhibitors.

Journal: Cancer research 20100701

Title: A rapid and sensitive method for determination of veliparib (ABT-888), in human plasma, bone marrow cells and supernatant by using LC/MS/MS.

Journal: Journal of pharmaceutical and biomedical analysis 20100501

Title: Crystal structure of the catalytic domain of human PARP2 in complex with PARP inhibitor ABT-888.

Journal: Biochemistry 20100216

Title: Plasma and cerebrospinal fluid pharmacokinetics of ABT-888 after oral administration in non-human primates.

Journal: Cancer chemotherapy and pharmacology 20100201

Title: Simultaneous determination of ABT-888, a poly (ADP-ribose) polymerase inhibitor, and its metabolite in human plasma by liquid chromatography/tandem mass spectrometry.

Journal: Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 20100201

Title: Poly(adp-ribose) polymerase inhibitors: a novel drug class with a promising future.

Journal: Cancer journal (Sudbury, Mass.) 20100101

Title: Emergence of rationally designed therapeutic strategies for breast cancer targeting DNA repair mechanisms.

Journal: Breast cancer research : BCR 20100101

Title: ABT-888 confers broad in vivo activity in combination with temozolomide in diverse tumors.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20091201

Title: Synthesis and evaluation of a new generation of orally efficacious benzimidazole-based poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors as anticancer agents.

Journal: Journal of medicinal chemistry 20091112

Title: Immunohistochemical detection of poly(ADP-ribose) polymerase inhibition by ABT-888 in patients with refractory solid tumors and lymphomas.

Journal: Cancer biology & therapy 20091101

Title: Role of Phase 0 trials in drug development.

Journal: Future medicinal chemistry 20091101

Title: Acquired resistance to combination treatment with temozolomide and ABT-888 is mediated by both base excision repair and homologous recombination DNA repair pathways.

Journal: Molecular cancer research : MCR 20091001

Title: Poly(ADP-ribose) polymerase inhibitor ABT-888 potentiates the cytotoxic activity of temozolomide in leukemia cells: influence of mismatch repair status and O6-methylguanine-DNA methyltransferase activity.

Journal: Molecular cancer therapeutics 20090801

Title: Phase 0 trials: a platform for drug development?

Journal: Lancet (London, England) 20090718

Title: Phase 0 clinical trials: an answer to drug development stagnation?

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20090601

Title: Phase 0 clinical trial of the poly (ADP-ribose) polymerase inhibitor ABT-888 in patients with advanced malignancies.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20090601

Title: Phase 0 trials for anticancer drug development.

Journal: Nature reviews. Drug discovery 20090601

Title: Phase zero launch.

Journal: Nature biotechnology 20090601

Title: Effective sensitization of temozolomide by ABT-888 is lost with development of temozolomide resistance in glioblastoma xenograft lines.

Journal: Molecular cancer therapeutics 20090201

Title: 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.

Journal: Journal of medicinal chemistry 20090122

Title: 94th RSNA Annual Meeting.

Journal: The Lancet. Oncology 20090101

Title: Preclinical modeling of a phase 0 clinical trial: qualification of a pharmacodynamic assay of poly (ADP-ribose) polymerase in tumor biopsies of mouse xenografts.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20081101

Title: An enzyme-linked immunosorbent poly(ADP-ribose) polymerase biomarker assay for clinical trials of PARP inhibitors.

Journal: Analytical biochemistry 20081015

Title: 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.

Journal: Molecular cancer research : MCR 20081001

Title: Liquid chromatography-mass spectrometric assay for the quantitation in human plasma of ABT-888, an orally available, small molecule inhibitor of poly(ADP-ribose) polymerase.

Journal: Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 20080901

Title: A novel poly(ADP-ribose) polymerase inhibitor, ABT-888, radiosensitizes malignant human cell lines under hypoxia.

Journal: Radiotherapy and oncology : journal of the European Society for Therapeutic Radiology and Oncology 20080801

Title: Phase 0 trials: an industry perspective.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20080615

Title: Patient perspectives on phase 0 clinical trials.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20080615

Title: Poly (ADP-ribose) polymerase activity regulates apoptosis in HeLa cells after alkylating DNA damage.

Journal: Cancer biology & therapy 20080601

Title: The PARP inhibitor, ABT-888 potentiates temozolomide: correlation with drug levels and reduction in PARP activity in vivo.

Journal: Anticancer research 20080101

Title: Inhibition of poly(ADP-ribose) polymerase enhances cell death and improves tumor growth delay in irradiated lung cancer models.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20070515

Title: ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20070501

Title: Donawho CK, 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 May 1;13(9):2728-37.

Title: Du Y, et al. Blocking c-Met-mediated PARP1 phosphorylation enhances anti-tumor effects of PARP inhibitors. Nat Med. 2016 Feb;22(2):194-201.

Title: Liu F, et al. Effects of poly (ADP-ribose) polymerase-1 (PARP-1) inhibition on sulfur mustard-induced cutaneous injuries in vitro and in vivo. PeerJ. 2016 Apr 4;4:e1890.

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