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ABT-888 (Veliparib)Potent PARP inhibitor

ABT-888 (Veliparib)

Catalog No. A3002
Size Price Stock Qty
Evaluation Sample $28.00 In stock
5mg $54.00 In stock
10mg $77.00 In stock
50mg $231.00 In stock
200mg $678.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Nassour J, Martien S, et al."Defective DNA single-strand break repair is responsible for senescence and neoplastic escape of epithelial cells." Nat Commun. 2016 Jan 29;7:10399. PMID:26822533

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Chemical structure

ABT-888 (Veliparib)

Related Biological Data

ABT-888
ABT-888 enhances the antitumor activity of temozolomide in the rat 9L glioma orthotopic model. Tumor cells were inoculated into rat brain as described in Materials and Methods. The vehicle for the temozolomide and ABT-888 was saline. ABT-888 was administered at 25 mg/kg/dose, bd, orally, on days 2 to 17. Starting on day 4, temozolomide was administered at 17.5 mg/kg, qd, orally, on day 4 to 8 at 2 h post the morning dose of ABT-888.

Related Biological Data

ABT-888

Biological Activity

Veliparib (ABT-888) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM, respectively.
Targets PARP1 PARP2        
IC50 5.2 nM (Ki) 2.9 nM (Ki)        

Protocol

Cell experiment:

Cell lines

HCT-116 and HT-29 cell lines

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reacting condition

4 μM; 24 h

Applications

In HCT-116 and HT-29 cell lines, the ability of ABT-888 to synergize the effect of the anti-cancer agents, SN38 or oxaliplatin, was determined using the SRB assay. PARP activity was significantly reduced in samples treated with SN38 in combination with ABT-888 (>4 fold at 24 h).

Animal experiment:

Animal models

Female nude athymic mice

Dosage form

12.5 mg/kg; oral gavage twice daily in 6-hour intervals.

Application

HCT116 xenografts were established in 5- to 6-week-old female nude athymic mice by subcutaneous flank injections of 200 mL cell suspension (5*106cells) per flank. This triple-therapy group (RT, CPT-11, and ABT) showed a significantly longer tumor growth delay (TGD) when compared with the tumors treated with RT and CPT-11 but no ABT-888, which had a mean TGD of 14.21 days.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Davidson D, Wang Y, Aloyz R, et al. The PARP inhibitor ABT-888 synergizes irinotecan treatment of colon cancer cell lines[J]. Investigational new drugs, 2013, 31(2): 461-468.

[2] Shelton J W, Waxweiler T V, Landry J, et al. In vitro and in vivo enhancement of chemoradiation using the oral parp inhibitor ABT-888 in colorectal cancer cells[J]. International Journal of Radiation Oncology* Biology* Physics, 2013, 86(3): 469-476.

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Chemical Properties

Cas No. 912444-00-9 SDF Download SDF
Synonyms ABT-888,ABT 888,ABT888,Veliparib
Chemical Name 1-[3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one
Canonical SMILES CC1(CCCN1)C2=NC3=C(C=CC=C3N2)C(=O)N
Formula C13H16N4O M.Wt 244.3
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

View Related Products By Research Topics

Research Update

2. The PARP inhibitor ABT-888 synergizes irinotecan treatment of colon cancer cell lines. Invest New Drugs. 2013 Apr;31(2):461-8. doi: 10.1007/s10637-012-9886-7. Epub 2012 Oct 9.
Abstract
Treatments of ABT-888 (0.125 μΜ) with irinotecan and ABT-888 (0.5-4 μM) both exhibited synergistic effect against colon cancer cell lines, in which the synergy of ABT-888/irinotecan is correlated with the degree of PARP1 inhibition and results in increased G2/M cell cycle arrest and increased DNA damage after 24 h and increased apoptosis after 48 h.
4. Enhancement of synthetic lethality via combinations of ABT-888, a PARP inhibitor, and carboplatin in vitro and in vivo using BRCA1 and BRCA2 isogenic models. Mol Cancer Ther. 2012 Sep;11(9):1948-58. doi: 10.1158/1535-7163.MCT-11-0597. Epub 2012 Jul 9.
Abstract
ABT-888/carboplatin treatment exhibits a stronger ability to kill or inhibit proliferation of Brca/BRCA-deficient cells than cisplatin or carboplatin alone, which delayed tumor growth in Brca2 xenografts and induced DNA damage and apoptosis.
5. Phase I study of PARP inhibitor ABT-888 in combination with topotecan in adults with refractory solid tumors and lymphomas. Cancer Res. 2011 Sep 1;71(17):5626-34. doi: 10.1158/0008-5472.CAN-11-1227. Epub 2011 Jul 27.
Abstract
The combination of ABT-888 (10 mg) and topotecan (0.6 mg/m2/d) was orally administered to enrolled patients twice a day for the first 5 days during a 21-day cycle, in which a >75% reduction in PAR levels, a >50% reduction in PBMCs and increased γH2AX response in CTC and PBMCs were observed in patients.

Background

ABT-888, also named as Veliparib, is poly (ADP-ribose) polymerase (PARP) inhibitor and has demonstrated excellent in vivo efficacy in a broad spectrum of preclinical tumor models in combination with a variety of cytotoxic agents. PARP is involved in DNA repair and elevated PARP levels can result in resistance to cytotoxic chemotherapy and radiation. So, PARP inhibitors hold promise as chemotherapy and radiation sensitizers. ABT-888 is also active on microsatellite instability (MSI) cell lines harboring mutations in both MRE11 and RAD50 genes compared to microsatellite stable (MSS) cell lines (wild-type for both genes).

Reference

Shivaani Kummar, Robert Kinders, Martin E. Gutierrez, Larry Rubinstein, Ralph E. Parchment, Lawrence R. Phillips, Jiuping Ji, Anne Monks, Jennifer A. Low, Alice Chen, Anthony J. Murgo, Jerry Collins, Seth M. Steinberg, Helen Eliopoulos, Vincent L. Giranda, Gary Gordon, Lee Helman, Robert Wiltrout, Joseph E. Tomaszewski and James H. Doroshow. Phase 0 Clinical Trial of the Poly (ADP-Ribose) Polymerase Inhibitor ABT-888 in Patients With Advanced Malignancies. Journal of Clinical Oncology. 2009; 27(16): 2705 – 11.

Xiaofeng Li, Juergen Delzer, Richard Voorman, Sonia M. de Morais and Yanbin Lao. Disposition and Drug-Drug Interaction Potential of Veliparib (ABT-888), a Novel and Potent Inhibitor of Poly (ADP-ribose) Polymerase. DRUG METABOLISM AND DISPOSITION. 2011; 39(7): 1161 – 69.

E. Vilar Sanchez, A. Chow, L. Raskin, M. D. Iniesta, B. Mukherjee and S. B. Gruber. Preclinical testing of the PARP inhibitor ABT-888 in microsatellite instable colorectal cancer. Journal of Clinical Oncology. 2009; 27(15S): 11028A.