Cellagentech/AG-014699 (PF-01367338, Rucaparib) | PARP1/2 inhibitor/C2401-5/5 mg (powder)-蚂蚁淘商城

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Cellagentech/AG-014699 (PF-01367338, Rucaparib) | PARP1/2 inhibitor/C2401-5/5 mg (powder)

2024-04-27

Product Description

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 4^oC desiccated, or store DMSO solution at -20^oC.

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