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Veliparib dihydrochloridePARP-1/PARP-2 inhibitor

Veliparib dihydrochloride

Catalog No. A3958
Size Price Stock Qty
10mM (in 1mL DMSO) $57.00 In stock
5mg $51.00 In stock
10mg $74.00 In stock
50mg $224.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Veliparib dihydrochloride

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)        

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Chemical Properties

Cas No. 912445-05-7 SDF Download SDF
Synonyms ABT-888 dihydrochloride;ABT888 dihydrochloride;ABT 888 dihydrochloride
Chemical Name 2-[(2R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide;dihydrochloride
Canonical SMILES CC1(CCCN1)C2=NC3=C(C=CC=C3N2)C(=O)N.Cl.Cl
Formula C13H18Cl2N4O M.Wt 317.21
Solubility Soluble in DMSO 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

Background

Veliparib dihydrochloride is a potent inhibitor of PARP-1 and PARP-2 with K (i) s of 5.2 and 2.9 nmol/L, respectively [1].
PARP is short of poly ADP ribose polymerase and is reported as an overexpressed enzyme in a variety of cancers. Since it has been revealed that several forms of cancer more independent on PARP compared with regular cells, which making PARP as an attractive target for cancer therapy. Many studies have shown that PARP inhibitors act as radio- and chemotherapy- sensitizers in preclinical studies using both in vitro and in vivo models [2] [3].
Veliparib dihydrochloride is a selective inhibitor of PARP. When tested with colon cancer cell lines HCT-116 and HT-29, using veliparib dihydrochloride as an adjuvant and combing with SN38 or Oxall resulted in increasing G2/M cell cycle arrest and increased levels of DNA damage via inhibiting PARP-1 and PARP-2 [4].
In mouse model with B16F10 murine melanoma cells injected subcutaneously, oral administration of veliparib dihydrochloride with temozolomide increased the efficacy at the concentration of 3.1 mg/kg/d~25 mg/kg/d and markedly slowed tumor progression. And similar results were achieved when tested with MX-1 breast xenograft model (BRCA1 deletion and BRCA2 mutation) or HCT-116 colon carcinoma model [1].
References:
[1].    Donawho, C.K., 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. 13(9): p. 2728-37.
[2].    Benafif, S. and M. Hall, An update on PARP inhibitors for the treatment of cancer. Onco Targets Ther, 2015. 8: p. 519-28.
[3].    Guillot, C., et al., PARP inhibition and the radiosensitizing effects of the PARP inhibitor ABT-888 in in vitro hepatocellular carcinoma models. BMC Cancer, 2014. 14: p. 603.
[4].    Davidson, D., et al., The PARP inhibitor ABT-888 synergizes irinotecan treatment of colon cancer cell lines. Invest New Drugs, 2013. 31(2): p. 461-8.