产品描述:
Rucaparib is a poly(ADP-ribose) polymerase 1 (PARP1) inhibitor.{20678} It reduces PARP1 activity in D283 Med medulloblastoma cells by 91.7% when used at a concentration of 1 µM. Rucaparib selectively inhibits the proliferation of MDA-MB-436 breast cancer cells expressing mutant BRCA1 (IC50s = 1.3 µM) over MCF-7 breast cancer cells expressing wild-type BRCA1 and BRCA2 (IC50s = 20.2 µM).{20679} It potentiates the growth inhibition induced by the DNA alkylating agent prodrug temozolomide (Item No. 14163) in D283 Med and D384 Med medulloblastoma cells when used at a concentration of 0.4 µM.{20678} In vivo, rucaparib (1 mg/kg per day) potentiates temozolomide-induced delays in tumor growth in D283 Med and D384 Med mouse xenograft models. Formulations containing rucaparib have been used in the treatment of BRCA mutation-associated, drug-resistant ovarian, fallopian tube, or primary peritoneal cancers.