| Identification | Back Directory | [Name]
Rucaparib Camsylate | [CAS]
1859053-21-6 | [Synonyms]
Rucaparib Camsylate
Rucaparib Camphosulfonate
8‐Fluoro‐2‐(4‐methylaminomethyl‐phenyl)‐1,3,4,5‐tetrahydro‐azepino[5,4,3‐cd] indol‐6‐one (S)‐camphorsulfonate Salt
Bicyclo[2.2.1]heptane-1-methanesulfonic acid, 7,7-dimethyl-2-oxo-, (1S,4R)-, 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) | [Molecular Formula]
C29H34FN3O5S | [MOL File]
1859053-21-6.mol | [Molecular Weight]
555.661 |
| Hazard Information | Back Directory | [Uses]
Rucaparib Camsylate is a novel DNA repair enzyme poly-ADP ribose polymerase-1 (PARP-1) inhibitor. | [Definition]
ChEBI:Rucaparib camsylate is a camphorsulfonate salt obtained by reaction of rucaparib with one molar equivalent of (1S,4R)-camphorsulfonic acid. It is an inhibitor of poly (ADP-ribose) polymerase and is used as monotherapy for advanced ovarian cancer and deleterious germline or somatic BRCA mutation. It has a role as an EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor. It is a camphorsulfonate salt and an azepinoindole. It contains a (S)-camphorsulfonate and a rucaparib(1+). | [Biological Activity]
Rucaparib is an inhibitor of the DNA repair enzyme poly-ADP ribose polymerase-1 (PARP-1). It has been found to have anticancer activity in a number of cancers and has been approved for treatment of previously treatedBRCA-mutant ovarian cancer. | [in vivo]
Rucaparib (AG014699) monocamsylate and AG14584 significantly increase Temozolomide toxicity. Rucaparib (1 mg/kg) monocamsylate significantly increases Temozolomide-induced body weight loss. Rucaparib (0.1 mg/kg) monocamsylate results in a 50% increase in the temozolomide-induced tumor growth delay[1].
Rucaparib (10 mg/kg for i.p. or 50, 150 mg/kg for p.o.; daily for 5 days per week for 6 weeks) monocamsylate significantly inhibits the growth of the tumor, and there is one complete tumor regression and two persistent partial regressions[2].
Rucaparib (150 mg/kg; p.o.; once per week for 6 weeks or three times per week for 6 weeks) monocamsylate has greatest antitumor effect with three complete regressions[2].
Rucaparib monocamsylate enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts[6].
| Animal Model: | Female CD-1 nude mice aged 10-12 weeks with Capan-1 cells[2] | | Dosage: | 10?mg/kg or 50, 150 mg/kg | | Administration: | 10?mg/kg for i.p. or 50, 150 mg/kg for p.o. | | Result: | Significantly inhibited the growth of the tumor.
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| [IC 50]
PARP-1: 1.4 nM (Ki); PARP-2; PARP-3 | [storage]
Store at -20°C |
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