AG-014699 (Rucaparib) is an intraveneously-administered, azepinone-indole-based inhibitor of PARP 1 and 2 (Ki = 1.4 nM) [1] AG-014699 induces selective cytotoxicity in tumor cells defective in homologous recombination repair (HRR) through BRCA1 and 2 mutation and non-BRCA mutated HRR defects. It is a potent chemosensitizer of temozolomide (3 to 10 fold) and topotecan (1.5 to 2.3 fold) antitumor activity in neuroblastoma cells. [2, 3]
Technical information:
| Chemical Formula: | C19H18FN3O.H3PO4 | |
| CAS #: | 459868-92-9 | |
| Molecular Weight: | 421.36 | |
| Purity: | > 98% | |
| Appearance: | Yellow | |
| Chemical Name: | 8-Fluoro-2-(4-methylaminomethyl-phenyl)-1,3,4,5-tetrahydro-azepino[5,4,3-cd]indol-6-one phosphate | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | AG-014699, AG014699, AG-14699, AG14699, AG-014447, PF-01367338, PF01367338, Rucaparib phosphate, Rucaparib |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | "Phase II trial of the Poly(ADP-ribose) polymerase (PARP) inhibitor AG-014699 in BRCA1 and 2 mutated advanced ovarian and breast cancer" Cancer Research UK / Newcastle Univ. Abstract 3104 |
| 2. | Thomas et al., Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial. Mol. Cancer. Ther. 2007, 6(3), 945-956. Pubmed ID:17363489 |
| 3. | Daniel 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. Pubmed ID:19174487 |
Other Information:
Product Specification (pdf) MSDS (pdf) Certificate of Analysis is available upon request.
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