Rucaparib

Rucaparib Structure
CAS No.
283173-50-2
Chemical Name:
Rucaparib
Synonyms
Rucaparib Base;8-fluoro-5-(4-((methylamino)methyl)phenyl)-2,3,4,6-tetrahydro-1H-azepino[5,4,3-cd]indol-1-one;Rikapbu;AG-14447;AG014447;Rucaparib;AG 014447;PF-01367388;AG 014447;AG014447;Rucaparib impurity
CBNumber:
CB51475507
Molecular Formula:
C19H18FN3O
Molecular Weight:
323.36
MOL File:
283173-50-2.mol
Modify Date:
2024/11/19 15:53:33

Rucaparib Properties

Melting point 187 - 189°C
Boiling point 625.2±55.0 °C(Predicted)
Density 1.281
storage temp. 2-8°C(protect from light)
solubility DMSO (Slightly), Methanol (Slightly)
form Yellow solid.
pka 14.10±0.20(Predicted)
color Pale Yellow to Yellow

SAFETY

Risk and Safety Statements

Symbol(GHS) 
GHS08
Signal word  Warning
Hazard statements  H361
Precautionary statements  P201-P202-P281-P308+P313-P405-P501

Rucaparib Chemical Properties,Uses,Production

Description

Rucaparib was approved in the US as an oral treatment for advanced ovarian cancer. Development of rucaparib began with collaborations between Cancer Research UK and Agouron Pharmaceuticals (later acquired by Pfizer). Global development rights for rucaparib were ultimately granted to Clovis Oncology via a licensing agreement from Pfizer. To qualify for treatment with rucaparib monotherapy, patients must demonstrate deleterious breast cancer (BRCA) mutation (germline and/or somatic)- associated advanced ovarian cancer and also must have previously been treated with two or more chemotherapy regimens. Rucaparib functions as a small molecule poly(ADPribose) polymerase (PARP) inhibitor, which plays an important role in DNA repair. This newly approved drug displays nanomolar potency against PARP-1, -2, and -3 enzymes, which translates into improved efficacy over alternative therapies such as olaparib or niraparib. Furthermore, rucaparib is also known to cause vasodilation, which is thought to induce tumor perfusion and increased accumulation of the drug in cancer cells. Although rucaparib shows higher cytotoxicity in cancer cells with mutation of BRCA1/2 genes and other DNA repair genes, reduced tumor growth was observed in mouse xenograft models of human cancers with and without BRCA mutations.Rucaparib is also being pursued as a treatment for breast cancer and has displayed promising initial results in trials for pancreatic cancer.

Uses

Rucaparib is PARP1 inhibitor. It can be used in biological study of chemical screening to identify drugs that enhance or mitigate cellular responses to antibody-toxin fusion proteins using human B cell precursor leukemia cells and cervical adenocarcinoma cells.

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Rucaparib Spectrum

8-FLUOR-2-{4-[(METHYLAMINO)METHYL]FENYL}-1,3,4,5-TETRAHYDRO-6HAZEPINO[5,4,3-CD]INDOOL-6-ON 8-fluoro-2-(4-((methylamino)methyl)phenyl)-4,5-dihydro-1H-azepino[5,4,3-cd]indol-6(3H)-one 6H-Pyrrolo[4,3,2-ef][2]benzazepin-6-one, 8-fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]- 8-Fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]-6H-pyrrolo[4,3,2-ef][2]benzazepin-6-one 8-Fluoro-2-[4-[(methylamino)methyl]phenyl]-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one Rucaparib rucaparib (PARP inhibitor) ORPHAN DRUG PF-01367388 Rucaparib impurity 6H-Pyrrolo[4,3,2-ef][2]benzazepin-6-one,8-fluoro-1,3,4,5-tet... AG-14447 Rucaparib free base AG-014699;PF-01367338; AG 014699;PF 01367338; AG014699;PF01367338 Rucaparib(AG-014447) Rikapbu AG014447 AG 014447;AG014447 AG 014447 8-fluoro-5-(4-((methylamino)methyl)phenyl)-2,3,4,6-tetrahydro-1H-azepino[5,4,3-cd]indol-1-one Rucaparib Base 8-Fluoro-2-[4-[(methylamino)methyl]phenyl]-4,5-dihydroazepino[5,4,3-cd]indol-6(3H)-one AG-14447|||PF-01367338|||AG014699 Rucaparib, 10 mM in DMSO 283173-50-2