Chemical Name: 2-[(2R)-2-Methyl-2-pyrrolidinyl]-1H-benzimidazole-4-carboxamide dihydrochloride
Biological ActivityHigh affinity PARP-2 and PARP-1 inhibitor (Ki 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.
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For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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
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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