6H-Pyrrolo[4,3,2-ef][2]benzazepin-6-one, 8-fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]- - Names and Identifiers
Name | 6H-Pyrrolo[4,3,2-ef][2]benzazepin-6-one,8-fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]-
|
Synonyms | Rikapbu AG014447 Rucaparib AG 014447 Rucaparib(AG-014447) 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 8-Fluoro-2-[4-[(methylamino)methyl]phenyl]-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one 6H-Azepino[5,4,3-cd]indol-6-one,8-fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]- 6H-Pyrrolo[4,3,2-ef][2]benzazepin-6-one,8-fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]- 6H-Pyrrolo[4,3,2-ef][2]benzazepin-6-one, 8-fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]-
|
CAS | 283173-50-2
|
EINECS | 814-445-0 |
6H-Pyrrolo[4,3,2-ef][2]benzazepin-6-one, 8-fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]- - Physico-chemical Properties
Molecular Formula | C19H18FN3O
|
Molar Mass | 323.36 |
Density | 1.281 |
Melting Point | 187 - 189°C |
Boling Point | 625.2±55.0 °C(Predicted) |
Solubility | DMSO (Slightly), Methanol (Slightly) |
Appearance | Yellow solid. |
Color | Pale Yellow to Yellow |
pKa | 14.10±0.20(Predicted) |
Storage Condition | 2-8°C(protect from light) |
In vitro study | Rucaparib is the most potent PARP inhibitor in enzyme assays (K i , 1.4 nM), and a possibleN-demethylation metabolite of AG14644. The radio-sensitization by Rucaparib is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib could target NF-κB activated by DNA damage and overcome toxicity observed with classical NF-κB inhibitors without compromising other vital inflammatory functions. Rucaparib inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilised D283Med cells. |
In vivo study | Rucaparib and AG14584 significantly (P < 0.05) increases temozolomide toxicity. Rucaparib (1 mg/kg) significantly increases temozolomide-induced body weight loss.Rucaparib (0.1 mg/kg) results in a 50% increase in the temozolomide-induced tumor growth delay. Rucaparib is not toxic but significantly enhances temozolomide-induced TGD in the DNA repair protein-competent D384Med xenografts. Pharmacokinetics studies also show that Rucaparib is detected in the brain tissue, which indicates that Rucaparib has potential in intra-cranial malignancy therapy. Rucaparib significantly potentiates the cytotoxicity of topotecan and temozolomide in NB-1691, SH-SY-5Y, and SKNBE (2c) cells. Rucaparib enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts. |
6H-Pyrrolo[4,3,2-ef][2]benzazepin-6-one, 8-fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]- - Introduction
6H-Pyrrolo[4,3,2-ef][2]benzazepin-6-one,8-fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]-is an organic compound. The following is a description of the properties, uses, preparation and safety information of the compound:
Nature:
-Appearance: A colorless or light yellow solid.
-Molecular formula: C17H17F2N3O.
-Molecular weight: 321.34g/mol.
-Melting point: About 120-122 ℃.
-Boiling point: About 520 ℃.
-Solubility: Soluble in organic solvents.
Use:
- 6H-Pyrrolo[4,3,2-ef][2]benzazepin-6-one,8-fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)) methyl]phenyl]-can be used to synthesize and study other organic compounds, such as drugs and dyes.
-It can also be used as an antibacterial agent, insecticide, preservative, etc.
Preparation Method:
-The preparation method of this compound is more complicated, and usually requires organic synthesis technology and chemical laboratory equipment.
-A common synthesis method is to initiate a sequence of chemical changes through reactions, including substitution, cyclization and oxidation reactions.
Safety Information:
- 6H-Pyrrolo[4,3,2-ef][2]benzazepin-6-one,8-fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)) the safety of methyl]phenyl]-has not been fully studied and evaluated.
-Appropriate safety precautions, such as wearing protective gloves, goggles and laboratory coats, are required when handling and using the compound.
-This compound may be toxic or irritating to humans and should be avoided by inhalation, ingestion or contact with skin.
-When using or handling the compound, follow laboratory safety procedures and comply with relevant regulations and guidelines.
Last Update:2024-04-09 01:59:57