215307-20-3

Basic information

• Product Name: 4-(Benzyloxy)-2-(4-fluorophenyl)-3-(4-pyridinyl)-1H-pyrrolo[2,3-b]pyridin-6-amine
• CAS NO: 215307-20-3
• Molecular Formula: C₂₅H₁₉FN₄O
• Molecular Weight: 410.45478
• Mol File: 215307-20-3.mol
• Article Data: 3

Chemical Properties

• CAS DataBase Reference: 4-(Benzyloxy)-2-(4-fluorophenyl)-3-(4-pyridinyl)-1H-pyrrolo[2,3-b]pyridin-6-amine(CAS DataBase Reference)
• NIST Chemistry Reference: 4-(Benzyloxy)-2-(4-fluorophenyl)-3-(4-pyridinyl)-1H-pyrrolo[2,3-b]pyridin-6-amine(215307-20-3)
• EPA Substance Registry System: 4-(Benzyloxy)-2-(4-fluorophenyl)-3-(4-pyridinyl)-1H-pyrrolo[2,3-b]pyridin-6-amine(215307-20-3)

Safety Data

• Hazardous Substances Data: 215307-20-3(Hazardous Substances Data)

Upstream product

• 18986-54-4 4?benzyloxy?2,6?diaminopyridine 
• 152122-41-3 2-(tert-butyldimethyl-silyloxy)-1-(4-fluorophenyl)-2-pyridin-4-yl-ethanone 
• 586-95-8 pyridine-4-methanol 
• 456-22-4 4-Fluorobenzoic acid 
• 18986-39-5 4?benzyloxy?2,6?dicarboethoxyamino pyridine 
• 18986-24-8 4?benzyloxy pyridine?2,6?dicarboxylic acid dihydrazide 
• 18986-14-6 4?benzyloxy pyridine?2,6?dicarboxylic acid diethyl ester 
• 68631-52-7 4-hydroxypyridine-2,6-dicarboxylic acid diethylester 
• 499-51-4 Chelidamic acid 
• 116332-54-8 4-fluoro-N-methoxy-N-methylbenzamide 
• 117423-41-3 4-((tert-butyldimethylsilyloxy)methyl)pyridine 

Relevant articles and documents

Development of a p38α-selective radioactive probe for qualitative diagnosis of cancer using SPECT

Objective: p38 mitogen-activated protein (MAP) kinase (p38α) has drawn attention as a new target molecule for the treatment and diagnosis of cancer, and its overexpression and activation have been reported in various types of cancer. In this study, a single photon emission computed tomography (SPECT) imaging probe of p38α was developed to noninvasively image p38α activity for effective qualitative diagnosis of cancer. Methods: Pyrrolepyridine derivatives, m-YTM and p-YTM, were designed and synthesized based on the structure of the p38α-selective inhibitor. Radioactive iodine-labeled m-YTM, [125I]m-YTM, was synthesized because m-YTM greatly inhibited the phosphorylation of p38α upon examining the inhibitory effects of the compounds. After investigating the binding affinity of [125I]m-YTM to the recombinant p38α, a saturation binding experiment using activated p38α and inactive p38α was performed to determine the binding site. Uptake of [125I]m-YTM into various cancer cell lines was investigated, and the pharmacokinetics was evaluated using tumor-bearing mice. Results: The inhibitory activity of m-YTM was approximately 13 times higher than that of SB203580, a p38α-selective inhibitor. The binding site of [125I]m-YTM was estimated to be the p38α activating site, similar to that of SB203580, because the [125I]m-YTM bound strongly to both activated p38α and inactive p38α. Various different cancer cells incorporated [125I]m-YTM; however, its accumulation was significantly reduced by treatment with SB203580. Pharmacokinetics study of [125I]m-YTM in B-16 tumor-bearing mice was examined which revealed high accumulation of radioactivity in tumor tissues. The ratios of radioactivity in the B-16 tumor to that in blood were 3.1 and 50 after 1 and 24?h, respectively. The ratio of radioactivity in the tumor to that in blood in the tumor-bearing mice generated using other cancer cell lines was also ≥ 1 at 1?h after the administration of the probe. Conclusions: This study suggests that [123I]m-YTM has potential as a p38α imaging probe effective for various cancer types.

Potent inhibitors of the MAP kinase p38

The MAP kinase p38 plays a key role in the biosynthesis of the inflammatory cytokines TNF-α and IL-1. We have developed a novel series of potent p38 inhibitors that could lead to new methods of treatment for inflammatory diseases such as rheumatoid arthritis and inflammatory bowel disease.