Cayman Rucaparib; Purity- Greater Than Or Equal To 98%; Size- 5 M

Poly(ADP-ribose) polymerases (PARPs) are activated by DNA single- and double-strand breaks and promote repair of DNA damage through the relaxation of chromatin and recruitment of other repair proteins.^1,2,3 Inhibition of PARP activity has been linked to synthetic lethality in cells with mutations in BRCA1 or BRCA2 and is used as a therapeutic strategy to selectively target cancers.^4,5 Rucaparib is a potent, cell-permeable inhibitor of PARP1 (K_i = <5 nM) that is used in clinical therapy to sensitize cancer cells to chemotherapy.^6,7 Rucaparib inactivates PARP activity in cells with homologous recombination DNA repair pathway mutations at LC₅₀ values ranging from 1.3-5.5 μM.⁷ At 25 mg/kg, rucaparib arrests tumor growth in mice bearing epigenetically silenced BRCA1 UACC3199 xenograft tumors.⁷ It has been shown to increase efficacy of temozolomide in medulloblastoma cells and xenografts.⁶

WARNING This product is not for human or veterinary use.