ChemicalBook--->CAS DataBase List--->459868-92-9

459868-92-9

459868-92-9 Structure

459868-92-9 Structure
IdentificationBack Directory
[Name]

PF-01367338
[CAS]

459868-92-9
[Synonyms]

CS-47
Rubraca
AG14699
AG-014699
PF-01367338
Rucaparib(AG-01)
AG014699 phosphate
AG-014699 phosphate
AG 014699 phosphate
PF-01367338/AG14699
Rucaparib phosphate
Rucaparib(AG-014699)
PF01367338 phosphate
AG-014699 (Rucaparib)
AG-014699;PF-01367338
PF-01367338 USP/EP/BP
Rucaparib ( PF-01367338)
Rucaparib phosphate salt
AG-014447 (as free base)
AG-14699 (as phosphate salt)
AG014699;RUCAPARIB PHOSPHATE
Rucaparib phosphate AG-014699
Rucaparib (AG-014699) phosphate
AG 014699 - PF 01367338 | Rucaparib
Rucaparib (AG-014699 , PF-01367338)
Rucaparib phosphate (AG-14699, PF-01367338)
Rucaparib (AG-014699,PF-01367338) phosphate
Rucaparib (phosphate)(AG-014699,PF-01367338)
AG-14699 (AS PHOSPHATE SALT); AG-014447 (AS FREE BASE); RUCAPARIB; PF-01367338; AG014699;
8-Fluoro-2-(4-((methylamino)methyl)phenyl)-4,5-dihydro-1H-azepino[5,4,3-cd]indol-6(3H)-one pho
8-Fluoro-2-(4-((methylamino)methyl)phenyl)-4,5-dihydro-1H-azepino[5,4,3-cd]indol-6(3H)-one phosphate
8-fluoro-5-(4-((methylamino)methyl)phenyl)-2,3,4,6-tetrahydro-1H-azepino[5,4,3-cd]indol-1-onephosphate
8-fluoro-5-(4-((methylamino)methyl)phenyl)-3,4-dihydro-2H-azepino[5,4,3-cd]indol-1(6H)-one phosphoric acid
8-Fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]-6H-pyrrolo[4,3,2-ef][2]benzazepin-6-one phosphate
6H-Pyrrolo[4,3,2-ef][2]benzazepin-6-one, 8-fluoro-1,3,4,5-tetrahydro-2-[4-[(MethylaMino)Methyl]phenyl]-, phosphate (1:1)
RUCAPARIB PHOSPHATE;AG014699 PHOSPHATE;PF01367338 PHOSPHATE;AG 014699 PHOSPHATE;PF 01367338 PHOSPHATE;AG-014699 PHOSPHATE;PF-01367338 PHOSPHATE
AG14699 (AS PHOSPHATE SALT); AG 14699; AG-14699; AG014447 (AS FREE BASE); AG-014447; AG 014447; PF01367338; PF-01367338; PF 01367338; RUCAPARIB; RUBRACA;
AG 014699 8-Fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]-6H-pyrrolo[4,3,2-ef][2]benzazepin-6-one phosphate
8-Fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]-6H-pyrrolo[4,3,2-ef][2]benzazepin-6-one phosphate Rucaparib(AG-014699)
[Molecular Formula]

C19H21FN3O5P
[MDL Number]

MFCD17010269
[MOL File]

459868-92-9.mol
[Molecular Weight]

421.37
Chemical PropertiesBack Directory
[storage temp. ]

Sealed in dry,Room Temperature
[solubility ]

Soluble in DMSO (up to 25 mg/ml).
[form ]

Yellow solid.
[color ]

Yellow
[Stability:]

Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Safety DataBack Directory
[Symbol(GHS) ]


GHS07,GHS02
[Signal word ]

Warning
[Hazard statements ]

H315-H319-H226
[Precautionary statements ]

P501-P240-P210-P233-P243-P241-P242-P264-P280-P370+P378-P337+P313-P305+P351+P338-P362+P364-P303+P361+P353-P332+P313-P403+P235
Hazard InformationBack Directory
[Description]

Rucaparib phosphate (459868-92-9) is a potent (Ki<5 nM) PARP1 inhibitor.1?Cytotoxic to human cancer cells or xenograft tumors with mutated or epigenetically silenced BRCA1/2.2?Demonstrates antiproliferative effects in 26 out of 39 ovarian cancer cell lines.3?Synergizes with other anticancer agents such as topotecan, carboplatin, doxorubicin, paclitaxel,3 and temozolomide.4?Ameliorates the cardiotoxicity of doxorubicin.5?Recently approved for human use by the FDA.
[Uses]

PARP inhibitor oncolytic
[References]

1) Thomas?et al.?(2007),?Preclinical selection of a n novel poly(ADP-ribose) polymerase inhibitor for clinical trial; Mol. Cancer Ther.,?6?945 2) Drew?et al.?(2011),?Therapeutic potential of poly(ADP-ribose) polymerase inhibitor AG014699 in human cancers with mutated or methylated BRCA1 or BRCA2; J. Natl. Cancer Inst.,?103?334 3) Ihnen?et al.?(2013),?Therapeutic potential of the poly(ADP-ribose) polymerase inhibitor rucaparib for the treatment of sporadic human ovarian cancer; Mol. Cancer Ther.,?12?1002 4) Plummer?et al.?(2013),?A phase II study of the potent PARP inhibitor, Rucaparib (PF-01367338, AG014699), with temozolomide in patients with metastatic melanoma demonstrating evidence of chemopotentiation; Cancer Chemother. Pharmacol.,?71?1191 5) Ali?et al.?(2011),?The clinically active PARP inhibitor AG014699 ameliorates cardiotoxicity but does not enhance the efficacy of doxorubicin, despite improving tumor perfusion and radiation response in mice; Mol. Cancer Ther.,?10?2320
Spectrum DetailBack Directory
[Spectrum Detail]

PF-01367338(459868-92-9)1HNMR
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