459868-92-9

Basic information

• Product Name: PF-01367338
• Synonyms: AG-014699;PF-01367338;AG14699;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 , PF-01367338);Rucaparib phosphate;AG-014699 (Rucaparib);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)
• CAS NO: 459868-92-9
• Molecular Formula: C19H18FN3O5P
• Molecular Weight: 418.3354842
• EINECS: -0
• Product Categories: Amines;Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Inhibitor;Inhibitors
• Mol File: 459868-92-9.mol
• Article Data: 1

Chemical Properties

• Boiling Point: 625.2 °C at 760 mmHg
• Flash Point: 331.9 °C
• Appearance: /
• Vapor Pressure: 1.5E-15mmHg at 25°C
• Storage Temp.: Sealed in dry,Room Temperature
• Solubility: Soluble in DMSO (up to 25 mg/ml).
• Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
• CAS DataBase Reference: PF-01367338(CAS DataBase Reference)
• NIST Chemistry Reference: PF-01367338(459868-92-9)
• EPA Substance Registry System: PF-01367338(459868-92-9)

Safety Data

• Hazardous Substances Data: 459868-92-9(Hazardous Substances Data)

Usage

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

InChI:InChI=1/C19H18FN3O.H3O4P/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;1-5(2,3)4/h2-5,8-9,21,23H,6-7,10H2,1H3,(H,22,24);(H3,1,2,3,4)

Downstream Products

• 283173-50-2 Rucaparib 

Relevant articles and documents

SALTS OF TRICYCLIC INHIBITORS OF POLY(ADP-RIBOSE) POLYMERASES

Pharmaceutically acceptable salts of compounds of the formula (I) below are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapeutics in treatment of cancers and the amelioration of the effects of stroke, head trauma, and neurodegener