1346242-81-6

Basic information

• Product Name: JNJ-42756493
• Synonyms: JNJ-42756493;Erdafitinib;Erdafitinib(JNJ-42756493);N-(3,5-dimethoxyphenyl)-N'-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine;N1-(3,5-Dimethoxyphenyl)-N2-(1-methylethyl)-N1-[3-(1-methyl-1H-pyrazol-4-yl)-6-quinoxalinyl]-1,2-ethanediamine;Suftalan Zine;N-(3,5-Dimethoxyphenyl)-N'-isopropyl-N-[3-(1-methyl-1H-pyrazol-4-yl)-6-quinoxalinyl]-1,2-ethanediamine;N1-(3,5-dimethoxyphenyl)-N2-isopropyl-N1-(3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl)ethane-1,2-diamine
• CAS NO: 1346242-81-6
• Molecular Formula: C₂₅H₃₀N₆O₂
• Molecular Weight: 446.5447
• Product Categories: API
• Mol File: 1346242-81-6.mol
• Article Data: 10

Chemical Properties

• Boiling Point: 662.3±55.0 °C(Predicted)
• Appearance: /
• Density: 1.20±0.1 g/cm3(Predicted)
• Storage Temp.: -20°C Freezer, Under inert atmosphere
• Solubility: DMSO (Slightly), Methanol (Slightly)
• PKA: 9.45±0.29(Predicted)
• CAS DataBase Reference: JNJ-42756493(CAS DataBase Reference)
• NIST Chemistry Reference: JNJ-42756493(1346242-81-6)
• EPA Substance Registry System: JNJ-42756493(1346242-81-6)

Safety Data

• Hazardous Substances Data: 1346242-81-6(Hazardous Substances Data)

Usage

Description

Erdafitinib is an oral pan-FGFR (1-4) inhibitor with has demonstrated promising activity in patients with metastatic or unresectable UC and other histologies (eg, cholangiocarcinoma) with FGFR alterations. It is used in the therapy of locally advanced, unresectable or metastatic urothelial carcinoma. Erdafitinib has been associated with a high rate of serum enzyme elevations during therapy, but has not been linked to cases of clinically apparent acute liver injury.

History

In early April of 2019, the US FDA approved Janssen Pharmaceutical Companies' brand name Balversa (erdafitinib) as the first-ever fibroblast growth factor receptor (FGFR) kinase inhibitor indicated for patients with locally advanced or metastatic urothelial carcinoma, with susceptible FGFR3 or FGFR2 genetic alterations, that has progressed during or following platinum-containing chemotherapy, including within 12 months of neoadjuvant or adjuvant platinum-containing chemotherapy. At the same time, the FDA also approved the therascreen FGFR RGQ RT-PCR Kit (Qiagen) for utilization as a companion diagnostic with erdafitinib for selecting patients for the indicated therapy.

Uses

Erdafitinib is a fibroblast growth factor receptor inhibitor.

Upstream product

• 1346245-10-0 C₂₃H₂₅N₅O₅S 
• 1380345-34-5 1-methyl-α-oxo-1H-pyrazole-4-acetaldehyde 
• 875-51-4 4-Bromo-2-nitroaniline 
• 1346245-08-6 N-(3,5-dimethoxyphenyl)-N-[2-[[(1,1-dimethylethyl)dimethylsilyl]oxy]ethyl]-3 -(1-methyl-1H-pyrazol-4-yl)-6-quinoxalinamine 
• 75-31-0 isopropylamine 
• 97-02-9 2,4-Dinitroanilin 
• 706819-66-1 2-bromo-1-(1-methyl-1H-pyrazol-4-yl)ethan-1-one 
• 1083325-87-4 7‐bromo‐2‐(1‐methyl‐1H‐pyrazol‐4‐yl)quinoxaline 
• 2895-21-8 2-chloro-N-isopropylacetamide 
• 1346242-78-1 C₂₂H₂₃N₅O₃ 
• 1346245-09-7 N-(2-(((1,1-dimethylethyl)dimethylsilyl)oxy)ethyl)-3,5-dimethoxyaniline 
• 1021002-43-6 2-(3,5-dimethoxylphenylamino)ethanol 
• 1346245-04-2 3-(1-methyl-1H-pyrazol-4-yl)-6-quinoxalinamine 

Downstream Products

• 1346245-63-3 C₃₆H₃₉N₇O₄ 
• 1346253-27-7 C₃₂H₃₅N₇O₄ 
• 1346411-44-6 C₂₈H₃₇N₇O₂ 
• 1346243-60-4 C₃₂H₃₇N₇O₂ 

Relevant articles and documents

SOLID STATE FORMS OF ERDAFITINIB SALTS AND PROCESSES FOR PREPARATION OF ERDAFITINIB

The present disclosure relates to solid state forms of Erdafitinib salts, processes for preparation thereof, processes for preparation of Erdafitinib and pharmaceutical compositions thereof.

Preparation method of 3-(1-methyl-1H-pyrazol-4-yl)-6-quinoxaline amine

The invention discloses a preparation method of erlotinib intermediate 3-(1-methyl-1H-pyrazol-4-yl)-6-quinoxaline amine. According to the preparation method of the invention, 2, 4-dinitroaniline is adopted as an initial raw material, and basic unit reactions such as substitution, reductive cyclization, oxidation, condensation and the like are sequentially carried out to obtain the target intermediate. The preparation process has the advantages of easily available raw materials, rapidness, convenience, economy and environmental protection, is suitable for large-scale production, and provides anew preparation way for industrialization of erlotinib.

Preparation method of Erdafitinib intermediate

The invention discloses a preparation method of an Erdafitinib intermediate 3-(1-methyl-1H-pyrazole-4-yl)-6-quinoxaline amine. The method comprises the steps of by using 2, 4-dinitroaniline as an initial raw material, sequentially carrying out condensation, reduction, cyclization and other basic unit reactions to obtain the target intermediate. The preparation process has the advantages of easilyavailable raw materials, rapidness, convenience, economy and environmental protection, is suitable for large-scale production, and provides a new preparation way for industrialization of Erdafitinib.