Catalog No.S1004 Synonyms: NSC 737664
Molecular Weight(MW): 244.29
Veliparib (ABT-888) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Phase 3.
Cited by 78 Publications
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|Description||Veliparib (ABT-888) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Phase 3.|
|Features||Increases the efficacy of common cancer therapies such as radiation and alkylating agents.|
ABT-888 is inactive to SIRT2 (>5 μM).  ABT-888 inhibits the PARP activity with EC50 of 2 nM in C41 cells.  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.  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. 
|In vivo||The oral bioavailability of ABT-888 is 56%-92% in mice, Sprague-Dawley rats, beagle dogs, and cynomolgus monkeys after oral administration.  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.  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. |
|In vitro||DMSO||17 mg/mL (69.58 mM)|
|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.
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Clinical Trial Information
|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|NCT03044795||Withdrawn||Drug: Veliparib||Cancer||University Medical Center Groningen|AbbVie|Dutch Cancer Society||November 2019||Phase 2|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||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|
|NCT01445522||Completed||Drug: ABT-888|Drug: Cyclophosphamide||Neoplasms|Lymphoma||National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)||December 3 2008||Phase 1|
|NCT00649207||Completed||Drug: ABT-888|Radiation: Whole Brain Radiation Therapy||Brain Diseases|Brain Neoplasms|Central Nervous System Diseases|Neoplasm Metastasis|Nervous System Neoplasms||AbbVie (prior sponsor Abbott)|AbbVie||March 2008||Phase 1|
|NCT00553189||Completed||Drug: ABT-888|Drug: Topotecan||Solid Tumors|Lymphomas||National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)||August 9 2007||Phase 1|
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