Formulation: A solid
Formal Name: (1S,4R)-7,7-dimethyl-2-oxo-bicyclo[2.2.1]heptane-1-methanesulfonic acid, compd. with 8-fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]-6H-pyrrolo[4,3,2-ef][2]benzazepin-6-one (1:1)
Purity: ≥98%
Formula Markup: C19H18FN3O • C10H16O4S
Formula Weight: 555,7
Shelf life (days): 1460
CAS Number: 1859053-21-6
Notes: 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.
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