Rucaparib (camsylate)

Rucaparib is a poly(ADP-ribose) polymerase 1 (PARP1) inhibitor. 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). It potentiates the growth inhibition induced by the DNA alkylating agent prodrug temozolomide (Cay-14163) in D283 Med and D384 Med medulloblastoma cells when used at a concentration of 0.4 µM. 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.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). CAS Number: 1859053-21-6. Synonyms: AG-014699, PF-01367338. Molecular Formula: C19H18FN3O . C10H16O4S. Formula Weight: 555.7. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Slightly Soluble, Methanol: Soluble, Water: Slightly Soluble. SMILES: O=C1C2=C3C(CCN1)=C(C4=CC=C(C=C4)CNC)NC3=CC(F)=C2.[H][C@@]5(C(C)6C)CC[C@@]6(CS(O)(=O)=O)C(C5)=O. InChi Code: InChI=1S/C19H18FN3O.C10H16O4S/c1-21-10-11-2-4-12(5-3-11)18-14-6-7-22-19(24)15-8-13(20)9-16(23-18)17(14)15,1-9(2)7-3-4-10(9,8(11)5-7)6-15(12,13)14/h2-5,8-9,21,23H,6-7,10H2,1H3,(H,22,24),7H,3-6H2,1-2H3,(H,12,13,14)/t,7-,10-/m.1/s1. InChi Key: INBJJAFXHQQSRW-STOWLHSFSA-N.