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Biological Activity:
A PARP 1 inhibitor with potential chemosensitizing, radiosensitizing and antineoplastic activities; selectively binds to PARP1 (Ki=1.4 nM) and inhibits PARP1-mediated DNA repair, thereby enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis.
* AG-014699 is the phosphate salt of AG 014447 (CAS 283173-50-2) and has improved aqueous solubility.
References: online 1 2 3 4
HD Thomas et al. Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial. Mol. Cancer Ther. 2007, 6(3), 945-56. [online]
P Plummer et al. Phase I study of the poly(ADP-ribose) polymerase inhibitor, AG014699, in combination with temozolomide in patients with advanced solid tumors. Clin Cancer Res. 2008, 14(23), 7917-23. [online]
M Ali etal. Vasoactivity of AG014699, a Clinically Active Small Molecule Inhibitor of Poly(ADP-ribose) Polymerase: a Contributory Factor to Chemopotentiation In vivo? Clin. Cancer Res. 2009, 15(19), 6106-6112. [online]
Chemical Name: 8-Fluoro-2-(4-methylaminomethyl-phenyl)-1,3,4,5-tetrahydro-azepino[5,4,3-cd]indol-6-one phosphate
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