Synonyms: AS-703026 | AS703026 | MSC1936369B
Compound class:
Synthetic organic
Comment: Pimasertib is an orally bioavailable small-molecule inhibitor of the mitogen-activated protein kinases MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity [4]. It binds to an allosteric site, distinct from the ATP binding site [2] and as such prevents activation rather than inhibiting catalysis.
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. Chang-Yew Leow C, Gerondakis S, Spencer A. (2013)
MEK inhibitors as a chemotherapeutic intervention in multiple myeloma. Blood Cancer J, 3: e105. [PMID:23524590] |
2. Goutopoulos A, Askew, BC, Bankston, D Clark, A, Dhanabal M, Dong R, Fischer D, Healey B, Jiang X, Josephson, K et al.. (2009)
AS703026: a novel allosteric MEK inhibitor. In: Proceedings of the 100th Annual Meeting of the American Association for Cancer Research; 2009 Apr 18-22; Denver, CO, Philadelphia (PA). AACR,: Abstract 4776. |
3. Kim K, Kong SY, Fulciniti M, Li X, Song W, Nahar S, Burger P, Rumizen MJ, Podar K, Chauhan D et al.. (2010)
Blockade of the MEK/ERK signalling cascade by AS703026, a novel selective MEK1/2 inhibitor, induces pleiotropic anti-myeloma activity in vitro and in vivo. Br J Haematol, 149 (4): 537-49. [PMID:20331454] |
4. Yoon J, Koo KH, Choi KY. (2011)
MEK1/2 inhibitors AS703026 and AZD6244 may be potential therapies for KRAS mutated colorectal cancer that is resistant to EGFR monoclonal antibody therapy. Cancer Res, 71 (2): 445-53. [PMID:21118963] |