Veliparib dihydrochloride is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM, respectively.
Veliparib 2HCl/维利帕尼二盐酸盐 细胞实验
Cell Line
Concentration
Treated Time
Description
References
D425GiL medulloblastoma cells
10 µM
10, 20, 40, 60, 80, 100, or 120 minutes
To assess the effect of Veliparib on the repair of radiation-induced DNA damage using the alkaline comet assay, results showed that Veliparib significantly delayed DNA damage repair.
Front Mol Biosci. 2021 Apr 29;8:633344.
D283Luc2 medulloblastoma cells
10 µM
14 days
To assess the effect of Veliparib on the colony-forming capacity of medulloblastoma cells using clonogenicity assays, results showed that Veliparib significantly impaired colony-forming capacity.
Front Mol Biosci. 2021 Apr 29;8:633344.
Primary mouse cortical neurons
1 µM
14 days
Prevented the α-syn PFF-mediated PARP activation and cell death
Science. 2018 Nov 2;362(6414):eaat8407.
D425 medulloblastoma cells
10 µM
24 hours
To assess the effect of Veliparib on the number of γH2AX and RPA32/RPA2 foci, results showed that Veliparib significantly increased the number of γH2AX foci, indicating increased DNA damage.
Front Mol Biosci. 2021 Apr 29;8:633344.
LNCaP cells
0-50 µM
3 days
To evaluate the sensitivity of PCa cells to Veliparib, results showed that Veliparib had no noticeable toxicity in all tested cells at concentrations under 50 µM.
J Exp Clin Cancer Res. 2018 Jul 16;37(1):153.
DU145 cells
0-50 µM
3 days
To evaluate the sensitivity of PCa cells to Veliparib, results showed that DU145 cells were more sensitive to Veliparib.
J Exp Clin Cancer Res. 2018 Jul 16;37(1):153.
Human liver lysosome lysate
0.5 µM
30 min, 2 hours, 24 hours
To investigate the rate of release of veliparib and its correlation with the chemical nature of the prodrugs.
ACS Med Chem Lett. 2023 Apr 24;14(5):652-657.
DU145, SF295
10 µM
72 hours
The cytotoxicity of three clinically relevant PARP inhibitors shows marked differences across different cell lines with MK-4827 and olaparib being the most cytotoxic and veliparib the least.
Cancer Res. 2012 Nov 1;72(21):5588-99.
D425GiL medulloblastoma cells
up to 25 µM
72 hours
To determine the effect of Veliparib on medulloblastoma cell viability, results showed minimal effect on cell viability at concentrations up to 25 µM.
Front Mol Biosci. 2021 Apr 29;8:633344.
CAPAN-1 cells
1, 10, 25 µM
Chromatin fractionation assays showed that UKTT15 exhibited an increased ability to trap PARP-1 on DNA compared to veliparib in MMS-treated CAPAN-1 cells.
Science. 2020 Apr 3;368(6486):eaax6367.
Veliparib 2HCl/维利帕尼二盐酸盐 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
NOD/Rag1−/− mice
D425GiL medulloblastoma xenograft model
Oral
12.5 mg/kg
Twice daily for 9 days
To assess the effect of Veliparib combined with radiotherapy in a medulloblastoma mouse model, results showed that combination therapy significantly increased survival.
Front Mol Biosci. 2021 Apr 29;8:633344.
Mice
Α-syn PFF injection model
Oral
125 mg/kg
Continuous administration
Reduced α-syn PFF-induced DA neuron loss
Science. 2018 Nov 2;362(6414):eaat8407.
Nude mice
DU145 xenograft model
Oral gavage
25 mg/kg/day
Once daily for 3 weeks
To validate the antitumor effect of Veliparib combined with SAHA, results showed that the combination therapy significantly inhibited the growth of xenografts.
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