639858-45-0

Usage

Uses

Used in Pharmaceutical Industry:
5-Amino-2,4-difluorobenzoic acid, 98% is used as a key intermediate for the synthesis of dual vascular endothelial growth factor receptor-2 (VEGFR-2) and fibroblast growth factor receptor-1 (FGFR-1) inhibitors. These inhibitors play a crucial role in the development of targeted therapies for various types of cancer, as they help in blocking the signaling pathways involved in tumor growth and angiogenesis.
5-AMino-2,4-difluorobenzoic acid, 98% is particularly useful in the development of small molecule inhibitors that can effectively target both VEGFR-2 and FGFR-1, making it a valuable asset in the fight against cancer. By inhibiting these receptors, the compound can potentially limit the growth of new blood vessels that supply nutrients to the tumor, thereby starving the cancer cells and preventing their proliferation.

Upstream product

• 153775-33-8 2,4-difluoro-5-nitro-benzoic acid 

Downstream Products

• 658085-51-9 5-amino-2,4-difluoro-N-methoxybenzamide 
• 639858-44-9 5-amino-2,4-difluoro-N-methylbenzamide 
• 125568-73-2 2,4-difluoro-5-aminobenzoic acid methyl ester 

Relevant academic research and scientific papers

Pyrrolotriazine kinase inhibitors

The present invention provides compounds of formula I, and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as anti-ca

Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5- (methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors

A series of substituted 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino) pyrrolo[2,1-f][1,2,4]-triazines was identified as potent and selective inhibitors of the tyrosine kinase activity of the growth factor receptors VEGFR-2 (Flk-1, KDR) and FGFR-1. The enzyme kinetics associated with the VEGFR-2 inhibition of compound 50 (Ki = 52 ± 3 nM) confirmed that the pyrrolo-[2,1-f][1,2,4]triazine analogues are competitive with ATP. Several analogues demonstrated low-nanomolar inhibition of VEGF- and FGF-dependent human umbilical vein endothelial cell (HUVEC) proliferation. Replacement of the C6-ester substituent of the pyrrolo[2,1-f][1,2,4]-triazine core with heterocyclic bioisosteres, such as substituted 1,3,5-oxadiazoles, afforded compounds with excellent oral bioavailability in mice (i.e., 50 Fpo = 79%). Significant antitumor efficacy was observed with compounds 44, 49, and 50 against established L2987 human lung carcinoma xenografts implanted in athymic mice. A full account of the synthesis, structure-activity relationships, pharmacology, and pharmacokinetic properties of analogues within the series is presented.

Heterocyclic inhibitors of kinases

The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.

PYRROLOTRIAZINE KINASE INHIBITORS

The present invention provides compounds of formula I, (I) and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as ant