894783-71-2

Usage

Uses

Used in Pharmaceutical Industry:
BIBF 1202 is used as an antitumor agent for its ability to inhibit the activity of VEGFR2, FGFR, and PDGFR, which play crucial roles in tumor angiogenesis, growth, and metastasis. This makes it a potential candidate for the treatment of various types of cancer.
Used in Cancer Treatment:
BIBF 1202 is used as a targeted therapy for cancer, specifically for inhibiting the VEGFR2 pathway, which is involved in tumor angiogenesis and growth. Its high potency and selectivity for VEGFR2 make it a promising option for the treatment of cancer.
Used in Drug Development:
BIBF 1202 serves as a valuable compound in drug development, as it can be further optimized and modified to improve its pharmacokinetic properties, bioavailability, and therapeutic efficacy. This can lead to the development of novel antitumor agents with enhanced potency and selectivity.

Upstream product

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• 676326-36-6 1-acetyl-2-oxo-2,3-dihydro-1H-indole-6-carboxylic acid methyl ester 
• 656247-17-5 nintedanib 
• 14192-26-8 2-oxo-2,3-dihydro-1H-indole-6-carboxylic acid methyl ester 
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• 2653-16-9 2-chloro-N-methyl-N-(4-nitrophenyl)acetamide 
• 100-15-2 N-methyl(p-nitroaniline) 
• 1027407-75-5 (Z)-1-acetyl-3-(ethoxy-phenyl-methylene)-2-oxo-2,3-dihydro-1H-indole-6-carboxylic acid methyl ester 

Relevant academic research and scientific papers

Harnessing affinity-based protein profiling to reveal a novel target of nintedanib

Nintedanib (BIBF1120), a triple angiokinase inhibitor, was first approved for idiopathic pulmonary fibrosis (IPF) therapy and is also efficacious for lung carcinoma, and interstitial lung diseases, far beyond its inhibition of VEGFR/PDGFR/FGFR. We identified tripeptidyl-peptidase 1 (TPP1) as one of the direct targets of nintedanib employing the affinity-based protein profiling (AfBPP) technique. This may be a new mechanism for nintedanib's role different from tyrosine kinase inhibition.

INDOLINONE DERIVATIVES AS INHIBITORS OF MATERNAL EMBRYONIC LEUCINE ZIPPER KINASE

The present disclosure relates to indolinone compounds, compositions, and methods for the inhibition of maternal embryonic leucine zipper kinase (MELK). The present disclosure further relates to indolinone compounds, compositions, and methods for the treatment or prevention of a cancer (for example, triple negative breast cancer).

Discovery of a potent inhibitor of MELK that inhibits expression of the anti-apoptotic protein Mcl-1 and TNBC cell growth

Despite recent advances in molecularly directed therapy, triple negative breast cancer (TNBC) remains one of the most aggressive forms of breast cancer, still without a suitable target for specific inhibitors. Maternal embryonic leucine zipper kinase (MELK) is highly expressed in TNBC, where level of overexpression correlates with poor prognosis and an aggressive disease course. Herein, we describe the discovery through targeted kinase inhibitor library screening, and structure-guided design of a series of ATP-competitive indolinone derivatives with subnanomolar inhibition constants towards MELK. The most potent compound, 17, inhibits the expression of the anti-apoptotic protein Mcl-1 and proliferation of TNBC cells exhibiting selectivity for cells expressing high levels of MELK. These studies suggest that further elaboration of 17 will furnish MELK-selective inhibitors with potential for development in preclinical models of TNBC and other cancers.

Medicaments for the Treatment or Prevention of Fibrotic Diseases

The present invention relates to the use of indolinones of general formula substituted in the 6 position, wherein R1 to R5 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof, as a medicament for the prevention or treatment of specific fibrotic diseases.