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283173-50-2

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

Molecular Formula: C19H18FN3O

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283173-50-2 - 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

283173-50-2 - Physico-chemical Properties

Molecular FormulaC19H18FN3O
Molar Mass323.36
Density1.281
Melting Point187 - 189°C
Boling Point625.2±55.0 °C(Predicted)
Solubility DMSO (Slightly), Methanol (Slightly)
AppearanceYellow solid.
ColorPale Yellow to Yellow
pKa14.10±0.20(Predicted)
Storage Condition2-8°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.

283173-50-2 - 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
283173-50-2
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283173-50-2
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