Veliparib dihydrochloride

Biological Activity

Veliparib dihydrochloride is a high affinity PARP-2 and PARP-1 inhibitor (K_i values are 2.9 and 5.2 nM, respectively). Inhibits repair of radiation-induced DNA damage and sensitizes lung cancer cells to radiation. Also increases autophagy and apoptosis in lung cancer cells. Enhances radiation-induced tumor growth delay in mice bearing lung tumor xenografts. Also chemosensitizer. Potentiates effects of temozolomide (Cat. No. 2706) in a mouse melanoma model. Orally bioavailable and brain penetrant.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Inhibition of poly(ADP-ribose) polymerase enhances cell death and improves tumor growth delay in irradiated lung cancer models.
   Albert et al.
   Clin.Cancer Res., 2007;13:3033
2. ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models.
   Donawho et al.
   Clin.Cancer Res., 2007;13:2728

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