Synonyms: AZ12607092 | AZD-7451 | AZD7451 | Example 6 [US8486966B2]
Compound class:
Synthetic organic
Comment: AZD7451 is a pan tropomyosin receptor kinase (TRK; also know as neurotrophic receptor tyrosine kinases or NTRKs) inhibitor [1]. It reached Phase 1 clinical development for anticancer potential, but the programme was discontinued. It was designed for the treatment of tumours that express oncogenic NTRK fusions [2-3]. The chemical structure of AZD7451 is identical to that which was submitted to the WHO for the INN utatrectinib (proposed INN list 126, Jan 2022).
![]() Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Davies A, Ioannidis S, Lamb M, Su M, Wang T, Zhang H-J. (2013)
9-(pyrazol-3-yl)-9H-purine-2-amine and 3-(pyrazol-3-yl) -3H-imidazo[4,5-B] pyridin-5-amine derivatives and their use for the treatment of cancer. Patent number: US8486966B2. Assignee: AstraZeneca AB. Priority date: 04/05/2007. Publication date: 17/07/2013. |
2. Ivanov SV, Panaccione A, Brown B, Guo Y, Moskaluk CA, Wick MJ, Brown JL, Ivanova AV, Issaeva N, El-Naggar AK et al.. (2013)
TrkC signaling is activated in adenoid cystic carcinoma and requires NT-3 to stimulate invasive behavior. Oncogene, 32 (32): 3698-710. [PMID:23027130] |
3. Tatematsu T, Sasaki H, Shimizu S, Okuda K, Shitara M, Hikosaka Y, Moriyama S, Yano M, Brown J, Fujii Y. (2014)
Investigation of neurotrophic tyrosine kinase receptor 1 fusions and neurotrophic tyrosine kinase receptor family expression in non-small-cell lung cancer and sensitivity to AZD7451 in vitro.. Mol Clin Oncol, 2 (5): 725-730. [PMID:25054037] |