AG-014699 phosphate

• CAT Number: I003606
• CAS Number: 459868-92-9
• Molecular Formula: C₁₉H₂₁FN₃O₅P
• Molecular Weight: 421.36
• Purity: ≥95%
• Synonyms: 8-fluoro-2-(4-((methylamino)methyl)phenyl)-4,5-dihydro-1H-azepino[5,4,3-cd]indol-6(3H)-one phosphate
• Target: PARP
• Solubility: DMSO: ≥ 33 mg/mL
• Storage: 3 years -20C powder
• IC50: 1.4 nM (Ki)

AG-014699 phosphate（Cat No.:I003606）, also known as Rucaparib phosphate, is a potent PARP (poly ADP-ribose polymerase) inhibitor. It works by inhibiting the PARP enzyme, which is involved in DNA repair, particularly single-strand break repair. By blocking PARP activity, AG-014699 induces synthetic lethality in cancer cells with deficient homologous recombination repair, such as BRCA1 or BRCA2 mutations, leading to cell death. This makes it a valuable therapeutic in cancer treatment, particularly for ovarian and breast cancers. Its phosphate form improves solubility and bioavailability for clinical applications in oncology.

Reference

[1]. Thomas HD, et al. Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial. Mol Cancer Ther, 2007, 6(3), 945-956.
[2]. Hunter JE, et al. NF-κB mediates radio-sensitization by the PARP-1 inhibitor, AG-014699. Oncogene, 2012, 31(2), 251-264.
[3]. Daniel RA, et al. Central nervous system penetration and enhancement of temozolomide activity in childhood medulloblastoma models by poly(ADP-ribose) polymerase inhibitor AG-014699. Br J Cancer, 2010, 103(10), 1588-1596.
[4]. Daniel RA, et al. Inhibition of poly(ADP-ribose) polymerase-1 enhances temozolomide and topotecan activity against childhood neuroblastoma. Clin Cancer Res, 2009, 15(4), 1241-1249.