Veliparib (ABT-888)

Name: Veliparib (ABT-888)
Brand: Selleck Chemicals
SKU: S1004
Rating: 5 (175 reviews)

For research use only.

Catalog No.S1004 Synonyms: NSC 737664

175 publications

CAS No. 912444-00-9

Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with K_i of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Veliparib increases autophagy and apoptosis. Phase 3.

Selleck's Veliparib (ABT-888) has been cited by 175 publications

Nature, 2019, 572(7768):254-259

PubMed: 31316209 ( click the link to review the publication )

Cancer Cell, 2019, 35(6):851-867

PubMed: 31185210 ( click the link to review the publication )

Nature, 2018, 559(7713):285-289

PubMed: 29973717 ( click the link to review the publication )

Nature, 2018, 559(7713):279-284

PubMed: 29950726 ( click the link to review the publication )

Cancer Discov, 2018, 8(8):988-1005

PubMed: 29880585 ( click the link to review the publication )

Cancer Cell, 2018, 33(3):401-416

PubMed: 29533782 ( click the link to review the publication )

Nature, 2017, 5;541(7635):87-91.

PubMed: 28002403 ( click the link to review the publication )

Cell, 2016, 167(1):233-247

PubMed: 27662091 ( click the link to review the publication )

Cell Metab, 2014, 19(6):1034-41

PubMed: 24814482 ( click the link to review the publication )

Sci Adv, 2021, 7(11)eabe9446

PubMed: 33712463 ( click the link to review the publication )

Mol Neurobiol, 2021, 10.1007/s12035-021-02371-4

PubMed: 33788167 ( click the link to review the publication )

Mol Med Rep, 2021, 23(1)40

PubMed: 33179075 ( click the link to review the publication )

Cell Death Differ, 2021, 10.1038/s41418-020-00733-4

PubMed: 33531658 ( click the link to review the publication )

Cancer Lett, 2021, S0304-3835(21)00092-6

PubMed: 33652085 ( click the link to review the publication )

Int J Mol Sci, 2021, 22(4)1638

PubMed: 33562002 ( click the link to review the publication )

Nat Commun, 2021, 12(1):736

PubMed: 33531508 ( click the link to review the publication )

Mol Cell, 2020, S1097-2765(20)30902-3

PubMed: 33412112 ( click the link to review the publication )

Mol Cell, 2020, S1097-2765(20)30898-4

PubMed: 33333017 ( click the link to review the publication )

Nat Commun, 2020, 11(1):5775

PubMed: 33188175 ( click the link to review the publication )

Nat Commun, 2020, 11(1):752

PubMed: 32029722 ( click the link to review the publication )

Nat Commun, 2020, 1;11(1):2174

PubMed: 32358582 ( click the link to review the publication )

Sci Adv, 2020, 22;6(17):eaaz3221

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Genome Med, 2020, 18;12(1):17

PubMed: 32070411 ( click the link to review the publication )

Cell Rep, 2020, 33(5):108347

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Aging Cell, 2020, 19(6):e13163

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Elife, 2020, 9e60637

PubMed: 32844745 ( click the link to review the publication )

Oncogene, 2020, 39(14):2905-2920

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Am J Cancer Res, 2020, 10(8):2649-2676

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Mol Cancer Res, 2020, 10.1158/1541-7786.MCR-19-0507

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DNA Repair (Amst), 2020, 85:102749

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Biochem Pharmacol, 2020, S0006-2952(20)30595-5

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Sci Rep, 2020, 10(1):15086

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Sci Rep, 2020, 10(1):3836

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Front Pharmacol, 2020, 11:610205

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Biochemistry, 2020, 10.1021/acs.biochem.0c00256

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SLAS Discov, 2020, 25(3):241-252

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Dis Markers, 2020, 2020:8259820

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Sci Rep, 2020, 10(1):9775

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Oncol Lett, 2020, 19(4):2629-2638

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Int J Radiat Oncol Biol Phys, 2020, 10.1016/j.ijrobp.2020.01.030

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Nat Commun, 2020, 11(1):3391

PubMed: 32636369 ( click the link to review the publication )

Transl Oncol, 2020, 13(11):100834

PubMed: 32688248 ( click the link to review the publication )

Nucleic Acids Res, 2020, gkaa590

PubMed: 32667640 ( click the link to review the publication )

Cell Rep, 2020, 32(2):107884

PubMed: 32668240 ( click the link to review the publication )

Sci Signal, 2020, 13(645):eaba8091

PubMed: 32817374 ( click the link to review the publication )

Mol Cell, 2020, 80(5):862-875.e6

PubMed: 33275888 ( click the link to review the publication )

Nat Commun, 2020, 11(1):6118

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Oncotarget, 2020, 11(23):2141-2159

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Nat Microbiol, 2019, 4(11):1872-1884

PubMed: 30988430 ( click the link to review the publication )

Mol Cell, 2019, 75(1):117-130

PubMed: 31101499 ( click the link to review the publication )

Nat Commun, 2019, 10(1):2910

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Nat Commun, 2019, 10(1):1307

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Nat Commun, 2019, 10(1):4632

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Nat Chem Biol, 2019, 15(12):1223-1231

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Nat Commun, 2019, 10(1):5654

PubMed: 31827085 ( click the link to review the publication )

Nat Commun, 2019, 10(1):4196

PubMed: 31519936 ( click the link to review the publication )

Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-2549

PubMed: 31852834 ( click the link to review the publication )

Int J Cancer, 2019, 10.1002/ijc.32558

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Cell Mol Life Sci, 2019, 76(10):2015-2030

PubMed: 30725116 ( click the link to review the publication )

Cancers (Basel), 2019, 12(1)

PubMed: 31861350 ( click the link to review the publication )

Clin Epigenetics, 2019, 11(1):4

PubMed: 30616689 ( click the link to review the publication )

Mol Ther Nucleic Acids, 2019, 17:701-713

PubMed: 31422287 ( click the link to review the publication )

Stem Cells, 2019, 37(1):42-53

PubMed: 30353615 ( click the link to review the publication )

Mol Cancer Ther, 2019, 10.1158/1535-7163.MCT-19-0474

PubMed: 31597711 ( click the link to review the publication )

Sci Rep, 2019, 9(1):3309

PubMed: 30824778 ( click the link to review the publication )

Cancer Chemother Pharmacol, 2019, 84(6):1241-1256

PubMed: 31541266 ( click the link to review the publication )

PLoS One, 2019, 14(8):e0213130

PubMed: 31408463 ( click the link to review the publication )

Biochem Biophys Res Commun, 2019, 510(4):501-507

PubMed: 30737031 ( click the link to review the publication )

Biochem Biophys Res Commun, 2019, 10.1016/j.bbrc.2019.10.141

PubMed: 31679697 ( click the link to review the publication )

JCI Insight, 2019, 4(4)

PubMed: 30830864 ( click the link to review the publication )

Cancer Immunol Res, 2019,

PubMed: 30401677 ( click the link to review the publication )

Acta Neuropathol Commun, 2018, 6(1):84

PubMed: 30157956 ( click the link to review the publication )
J Clin Invest, 2018, 128(7):2951-2965

PubMed: 29649003 ( click the link to review the publication )

Nat Commun, 2018, 9(1):176

PubMed: 29330466 ( click the link to review the publication )

Nat Commun, 2018, 9(1):967

PubMed: 29511213 ( click the link to review the publication )

EMBO J, 2018, 37(14)

PubMed: 29875130 ( click the link to review the publication )

EMBO Rep, 2018, 19(10):e46783

PubMed: 30291165 ( click the link to review the publication )

Elife, 2018, 7

PubMed: 30088474 ( click the link to review the publication )

J Exp Clin Cancer Res, 2018, 37(1):153

PubMed: 30012171 ( click the link to review the publication )

Cell Death Dis, 2018, 9(9):931

PubMed: 30209297 ( click the link to review the publication )

Cell Chem Biol, 2018, 25(12):1547-1553

PubMed: 30344052 ( click the link to review the publication )

Mol Oncol, 2018, 12(4):561-576

PubMed: 29465803 ( click the link to review the publication )

J Immunol, 2018,

PubMed: 29445007 ( click the link to review the publication )

J Pharmacol Exp Ther, 2018, 365(1):117-126

PubMed: 29339456 ( click the link to review the publication )

Biochem Biophys Res Commun, 2018, 500(2):333-338

PubMed: 29654761 ( click the link to review the publication )

SLAS Discov, 2018, 23(6):545-553

PubMed: 29676938 ( click the link to review the publication )

DNA Repair (Amst), 2018, 64:1-9

PubMed: 29459202 ( click the link to review the publication )

Nucleic Acids Res, 2018, 46(2):804-822

PubMed: 29216372 ( click the link to review the publication )

Genes Dev, 2017, 31(3):318-332

PubMed: 28242626 ( click the link to review the publication )

Cancer Lett, 2017, 386:131-140

PubMed: 27894958 ( click the link to review the publication )

Mol Cancer Ther, 2017, 16(12):2892-2901

PubMed: 28958991 ( click the link to review the publication )

Invest New Drugs, 2017, 35(3):251-259

PubMed: 28111726 ( click the link to review the publication )

PLoS One, 2017, 12(9):e0184619

PubMed: 28886188 ( click the link to review the publication )

Oncotarget, 2017, 8(53):90842-90851

PubMed: 29207607 ( click the link to review the publication )

Oncotarget, 2017, 8(40):68707-68720

PubMed: 28978150 ( click the link to review the publication )

Oncotarget, 2017, 8(61):103931-103951

PubMed: 29262611 ( click the link to review the publication )
EMBO Rep, 2016, 17(11):1609-1623

PubMed: 27596623 ( click the link to review the publication )

Cell Rep, 2016, 17(9):2367-2381

PubMed: 27880910 ( click the link to review the publication )

Cell Death Dis, 2016, 7:e2302

PubMed: 27441654 ( click the link to review the publication )

PLoS Genet, 2016, 12(9):e1006279

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Bioinformatics, 2016, 32(12):i253-i261

PubMed: 27307624 ( click the link to review the publication )

Mol Cancer Ther, 2016, 15(10):2302-2313

PubMed: 27474148 ( click the link to review the publication )

Mol Cancer Ther, 2016, 15(12):3087-3096

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Biochim Biophys Acta, 2016, 1863(12):3027-3039

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Neuropharmacology, 2016, 110(Pt A):287-296

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Cancer Gene Ther, 2016, 23(10):348-354

PubMed: 27632933 ( click the link to review the publication )

Mol Pharmacol, 2016, 90(2):65-79

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Analyst, 2016, 141(8):2454-62

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Toxicol Lett, 2016, 244:56-71

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PLoS One, 2016, 11(5):e0155711

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Nucl Med Biol, 2016, 43(12):752-758

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Oncotarget, 2016, 7(20):28765-82

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Mutat Res, 2016, 790:31-40

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Nucleic Acids Res, 2016, 44(3):1161-78

PubMed: 26578593 ( click the link to review the publication )

Oncotarget, 2016, 7(29):44950-44965

PubMed: 27391435 ( click the link to review the publication )

Oncotarget, 2016, 7(12):13984-4001

PubMed: 26910887 ( click the link to review the publication )

Oncotarget, 2016, 7(7):7701-14

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Sci Adv, 2015, 1:e1400203

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Elife, 2015, 4

PubMed: 26374986 ( click the link to review the publication )

Mol Cancer Ther, 2015, 14(11):2560-8

PubMed: 26351319 ( click the link to review the publication )
Mol Cancer Ther, 2015, 14(12):2818-30

PubMed: 26438158 ( click the link to review the publication )

Mol Cancer Ther, 2015, 10.1158/1535-7163.MCT-14-0810

PubMed: 25777962 ( click the link to review the publication )

Carcinogenesis, 2015, 36(8):832-40

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Hum Mol Genet, 2015, 24(12):3506-17

PubMed: 25788520 ( click the link to review the publication )

Frontiers in Oncology, 2015, 4:368

PubMed: 25566506 ( click the link to review the publication )

J Nutr Biochem, 2015, 26(12):1442-7

PubMed: 26350251 ( click the link to review the publication )

J Transl Med, 2015, 13:74

PubMed: 25886061 ( click the link to review the publication )

J Transl Med, 2015, 13(1):427

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Biochem J, 2015, 469(2):189-98

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Int J Oncol, 2015, 47(1):262-8

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Cancer Discov, 2015, 5(7):752-67

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Metabolomics, 2015, 11(6):1779-1791

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PLoS One, 2015, 10(5):e0126867

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Biochem Biophys Res Commun, 2015, 458(3):520-4

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J Breast Cancer, 2015, 18(4):329-38

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J Vet Emerg Crit Care (San Antonio), 2015, 25(4):528-37

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Sci Adv, 2015, 1(3):e1400203

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Clin Cancer Res, 2014, 20(10):2703-13

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J Cell Biol, 2014, 206(4):493-507

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Cell Rep, 2014, 9(3):829-41

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Cell Rep, 2014, 8(6):1808-18

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Oncogene, 2014, 8.559

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J Med Chem, 2014, 57(13):5579-601

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Mol Cancer Ther, 2014, 13(3):724-32

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Mol Cancer Ther, 2014, 13(6):1645-54

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Oral Oncol, 2014, S1368-8375(14)00163-8

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FEBS J, 2014, 281(16):3625-41

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Mol Cancer Res, 2014, 12(8):1128-39

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Biochim Biophys Acta, 2014, 1844(10):1765-72

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frontiers in genetic, 2014, 5:116-126

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J Biol Chem, 2014, 289(13):9247-53

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J Pharm Sci, 2014, 103(6):1913-20

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Transl Oncol, 2014, 10.1016/j.tranon.2014.04.003

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PLoS One, 2014, 9(7):e101844

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Asian Pac J Trop Med, 2014, 7(6):468-72

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Asian Pac J Trop Med, 2014, 468-472

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Oncotarget, 2014, 5(10):3115-29

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Oncotarget, 2014, 5(10):3023-8

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Assay Drug Dev Technol, 2014, 12(9-10):514-26

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Nucleic Acids Res, 2013, 41(7):4080-92

PubMed: 23449221 ( click the link to review the publication )

Clin Cancer Res, 2013, 19(18):5003-15

PubMed: 23881923 ( click the link to review the publication )

Cancer Res, 2013, 73(12):3683-91

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Cancer Lett, 2013, 343(2):217-23

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J Antimicrob Chemother, 2013, 12(7):529-34

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Carcinogenesis, 2013, 34(4):739-49

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Mol Cancer Res, 2013, 11(10):1179-92

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J Viral Hepat, 2013, 20(9):658-65

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PLoS One, 2013, 8(2):e55883

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Nucleic Acids Res, 2013, 41(15):7344-55

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Clin Cancer Res, 2012, 18(21):5878-87

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J Biol Chem, 2012, 287(52):43720-9

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Mol Pharmacol, 2012, 82(4):767-76

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Nucl Med Commun, 2012, 32(11):1046-51

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Cancer Res, 2011, 71(14):4944-54

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PLoS One, 2011, 6(12):e28862

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Purity & Quality Control

Choose Selective PARP Inhibitors

Biological Activity

Description

Features

Increases the efficacy of common cancer therapies such as radiation and alkylating agents.

Targets

PARP2 ^[1] (Cell-free assay)	PARP1 ^[1] (Cell-free assay)
2.9 nM(Ki)	5.2 nM(Ki)

In vitro

ABT-888 is inactive to SIRT2 (>5 μM). ^[1] ABT-888 inhibits the PARP activity with EC50 of 2 nM in C41 cells. ^[2] ABT-888 could decrease the PAR levels in both irradiated and nonirradiated H460 cells. ABT-888 also reduces clonogenic survival and inhibits DNA repair by PARP-1 inhibition in H460 cells. ABT-888 increases apoptosis and autophagy in H460 cells when combination with radiation. ^[3] ABT-888 also inhibits PARP activity in H1299, DU145 and 22RV1 cells and the inhibition is independent of p53 function. ABT-888 (10 μM) suppresses the surviving fraction (SF) by 43% in the clonogenic H1299 cells. ABT-888 shows effective radiosensitivity in oxic H1299 cells. Furthermore, ABT-888 could attenuate the SF of hypoxic-irradiated cells including H1299, DU145 and 22RV1. ^[4]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
C41	MWjLbY5ie2ViQYPzZZk>		MVKzNEBucW5?		MV7Jcohq[mm2aX;uJI9nKFCDUmCxJJdqfGhiRVO1NEBw\iByLkCwNkDPxE1?	MoPsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6OEi3OlAoRjF7OEi4O\|YxRC:jPh?=
Jurkat	MYnLbY5ie2ViQYPzZZk>		M2LlNlk3KGh?	MmHRSG1UVw>?	MmHRTY5pcWKrdHnvckBw\iCSQWLQNUBie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gZ4VtdCC4aXHibYxqfHlid3n0bEBGSzVyIH;mJFMh\|ryP	MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh3MEG5PUc,OjN6NUCxPVk9N2F-
Capan1	NVizSolXT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NYrJOFlVPzJiaB?=	MVrEUXNQ	MWrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFLSR2EzKGenbnWgcZV1[XSnZDDoeY1idiCFYYDhclEh[2WubIOge4l1cCCLQ{WwJI9nKDN7Lkeg{txO	MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN7OEO4N{c,OjR\|OUizPFM9N2F-
DT40	NVLXUZNRS3m2b4TvfIlkKEG\|c3H5		M{HQNlczKGh?	MnXTSG1UVw>?	NEPhcY9EgXSxdH;4bYNqfHliYXfhbY5{fCClaHnjb4VvKEKUQ1GyMYRm\mmlaXXueEBFXDRyIHPlcIx{	M3;uUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUKyOVg4Lz5{NEmyNlU5PzxxYU6=
ML-1	NIjDTVRCeG:ydH;0bYMhSXO\|YYm=	MlvWNk42KM7:TR?=	MWGyOEBp	MX\EUXNQ	M174OHN6dmW{Z3nzeIlk[WyueTDlcohidmOnczDUVmFKVC2rbnT1Z4VlKGGyb4D0c5NqeyCrbjDNUE0yKGOnbHzz	MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh7NUGzOUc,OjR6OUWxN\|U9N2F-
HCT-116	MXrLbY5ie2ViQYPzZZk>	M1\KUlAvPSEQvF2=	MYKyOEBp		NUP3SXJzWEGUUDDhZ5Rqfmm2eTDk[YNz\WG\|ZYO=	NWTjZVd7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOwOVQzOTNpPkKzNFU1OjF\|PD;hQi=>
UM-SCC1	NXfuXJNoS3m2b4TvfIlkKEG\|c3H5	MmHRNVAh\|ryP	NFe4NGozPCCq		MWjS[YR2[2W\|IITo[UBk\WyuII\pZYJqdGm2eR?=	NVTm[mJuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5NVI3OjBpPkKxPVEzPjJyPD;hQi=>
FaDu	NXTPXoFbS3m2b4TvfIlkKEG\|c3H5	NVf4[I9tOTBizszN	NYS5dotEOjRiaB?=		MoDBVoVlfWOnczD0bIUh[2WubDD2bYFjcWyrdIm=	M4rVXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOUGyOlIxLz5{MUmxNlYzODxxYU6=
PC-3	M2H1W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NH;lOFUyOCEQvF2=			MWfJcoR2[2W\|IHGgd4lodmmoaXPhcpQhcW6qaXLpeIlwdiCrbjDjc4xwdnliZn;ycYF1cW:wwrC=	NFXncm49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3NVkyOid-MkG1O\|E6OTJ:L3G+
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JVM-3	MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				M{jOOmlEPTB;M{WuOVg3QCEQvF2=	MnixQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVA3QDdzLze+V2FPT0WUPD;hQi=>
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JVM-2	MkH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MlT0TWM2OD12Mj65NlA4KM7:TR?=	M{TrOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUxPjh5MT:nQnNCVkeHUkyvZV4>
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BALL-1	M2XSUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MVjJR\|UxRTR\|Lkm1N\|Ih\|ryP	Mo\RQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVA3QDdzLze+V2FPT0WUPD;hQi=>
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Mo-T	MleyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MWjJR\|UxRTR3Lk[zPFkh\|ryP	M4PxfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUxPjh5MT:nQnNCVkeHUkyvZV4>
MHH-PREB-1	MlzUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				M2mwfGlEPTB;NEWuO\|U5PSEQvF2=	M1:2TlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUxPjh5MT:nQnNCVkeHUkyvZV4>
ALL-PO	M1Hrd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MkLwTWM2OD12Nz6zO\|kyKM7:TR?=	M1rHU\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUxPjh5MT:nQnNCVkeHUkyvZV4>
NCI-H510A	NXr0Z41vT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				M2r5d2lEPTB;NEeuPVA{PCEQvF2=	M1PD[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUxPjh5MT:nQnNCVkeHUkyvZV4>
ML-2	M3q3b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MX;JR\|UxRTR7Lke4OVYh\|ryP	NYKzV5k3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTB4OEexM{c,W0GQR1XSQE9iRg>?

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-STAT3 / STAT3 / p-AKT(S473) / p-AKT(T308) / p-ERK / p-p38; PubMed: 22678161 Breast Cancer Res Treat Effects of AG-014699, AZD-2281, ABT-888, or BSI-201 on the phosphorylation status of Stat3, Akt, ERK, and p38 in MDA-MB-468, MDA-MB-231, and Cal-51 cells after 72 h of treatment	22678161
Immunofluorescence	HuR; PubMed: 28687616 Cancer Res Immunofluorescent images of HuR (green) in MIA PaCa-2 cells treated with PARPi for 12hr. Nuclei were stained with DAPI. Magnification 40X. BRCA1; PubMed: 21917757 Int J Oncol Effects of ABT-888 and/or bortezomib on BRCA1 and RAD51 foci formation. BRCA1 and RAD1 foci induced by ABT-888 were completely resolved in cells cotreated with bortezomib. Image acquisition was performed with an epifluorescence microscope (BX51; Olympus) and multispectral color camera (Nuance FX; CRi) with a 60× or 100× magnification lens and oil immersion.	28687616 21917757
Growth inhibition assay	Cell viability (TNBC cell lines); PubMed: 27880910 Cell Rep BRCA-proficient TNBC cell lines were treated with veliparib in the absence and presence of dinaciclib, demonstrating reduced IC50 values in the presence of dinaciclib. Cell viability (melanoma cells); PubMed: 29956724 Int J Oncol Dose-dependent inhibitory effect of ABT-888 on melanoma cell proliferation. Human melanoma cell lines were exposed to diluents (control; CTRL) or increasing concentrations of ABT-888 for 72 h and their viability was assessed by MTT assay. Absorbance was detected at 540 nm with a microplate reader and data were expressed as a percentage of the CTRL. Data are the means ± SD of 3 experiments performed in triplicate. Statistical significance was calculated against the CTRL (P<0.05; *P<0.01).	27880910 29956724

In vivo

The oral bioavailability of ABT-888 is 56%-92% in mice, Sprague-Dawley rats, beagle dogs, and cynomolgus monkeys after oral administration. ^[1] ABT-888 (25 mg/kg i.p.) could improve tumor growth delay in a NCI-H460 xenograft model with well tolerated. Combination with radiation, ABT-888 decreases the tumor vessel formation. ^[3] ABT-888 reduces intratumor PAR levels by more than 95% at a dose of 3 and 12.5 mg/kg in A375 and Colo829 xenograft models and the suppression could be maintained over time. ^[4]

Protocol

Animal Research: ^[1]	- Collapse Animal Models: NCI-H460, H460, B16F10 and 9L xenografts in C57BL/6 mice Dosages: ~25 mg/kg Administration: Orally administered (Only for Reference)

References

[4] Kinders RJ, et al, Clin Cancer Res, 2008, 14(21), 6877-6885.

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Solubility (25°C)

In vitro	DMSO	17 mg/mL (69.58 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 0.5% methylcellulose+0.2% Tween 80 For best results, use promptly after mixing.	5 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download Veliparib (ABT-888) SDF

Molecular Weight	244.29
Formula	C₁₃H₁₆N₄O
CAS No.	912444-00-9
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	NSC 737664
Smiles	CC1(CCCN1)C2=NC3=C(C=CC=C3N2)C(=O)N

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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mg/kg

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Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

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Calculation results:

Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid 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 master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-01-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03044795	Withdrawn	Drug: Veliparib	Cancer	University Medical Center Groningen\|AbbVie\|Dutch Cancer Society	November 2019	Phase 2
NCT02723864	Active not recruiting	Drug: Veliparib + VX-970 + Cisplatin	Neoplasms	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	August 9 2017	Phase 1
NCT02483104	Completed	Drug: veliparib\|Drug: carboplatin\|Drug: paclitaxel	Ovarian Cancer	AbbVie	July 2015	Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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PARP Signaling Pathway Map

PARP Inhibitors with Unique Features

Selective PARP Inhibitors

AG-14361 : PARP1-selective, K_i<5 nM.
Selective PARP Inhibitors

UPF 1069 : PARP2-selective, IC50=0.3 μM.
Most Potent PARP Inhibitor

MK-4827 (Niraparib) : PARP1, IC50=3.8 nM; PARP2, IC50=2.1 nM.
PARP Inhibitor in Clinical Trial

Iniparib (BSI-201) : Phase III for solid tumors.
Newest PARP Inhibitor

BMN 673 : Novel PARP inhibitor with IC50 of 0.58 nM. Also a potent inhibitor of PARP-2, but does not inhibit PARG and highly sensitive to PTEN mutation.

Related PARP Products

G007-LK ^New

G007-LK is a potent and selective tankyrase inhibitor with IC50 of 46 nM and 25 nM for TNKS1/2, respectively.
NU1025 ^New

NU1025 (NSC 696807) is a potent PARP inhibitor with IC50 of 400 nM.
SCR7 ^New

SCR7 is a specific DNA Ligase IV inhibitor, which blocks nonhomologous end-joining (NHEJ). It increases the efficiency of HDR-mediated genome editing up to 19-fold using CRISPR/Cas9 in mammalian cells and mouse embryos.
Olaparib (AZD2281)

Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations.

Features:A potent PARP inhibitor (currently in late stage clinical trials).
Rucaparib (AG-014699) phosphate

Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with K_i of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3.

Features:The first PARP inhibitor used in clinical trials combined with temozolomide.
Talazoparib (BMN 673)

Talazoparib (BMN 673, LT-673) is a novel PARP inhibitor with IC50 of 0.57 nM for PARP1 in a cell-free assay. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3.

Features:Most potent and selective PARPi reported thus far.
Iniparib (BSI-201)

Iniparib (BSI-201, NSC-746045, IND-71677) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). Phase 3.
PJ34 HCl

PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.

Features:Water-soluble PARP1/2 inhibitor with >10,000-fold potentcy vs. 3-aminobenzamide (prototypical PARP inhibitor). Potential uses in cardiovascular diseases (stroke, cerebral ischemia, & myocardial ischemia).
AG-14361

AG14361 is a potent inhibitor of PARP1 with K_i of <5 nM in a cell-free assay. It is at least 1000-fold more potent than the benzamides.

Features:The 1st high-potency PARP-1 inhibitor with the specificity & in vivo activity to enhance chemotherapy and radiation therapy of human cancers.
A-966492

A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with K_i of 1 nM and 1.5 nM, respectively.

Features:A promising, structurally diverse benzimidazole analogue that is being further characterized preclinically.

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Veliparib (ABT-888)