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Synonyms: SAR-245408 | XL-147 | XL147
Compound class: Synthetic organic
Comment: Pilaralisib is an orally bioavailable small molecule inhibitor of the class I phosphatidylinositol 3 kinase (PI3K) family of lipid kinases, with potential antineoplastic activity [1-2].
Ligand Activity Visualisation Charts
These 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.✖
1. Chakrabarty A, Sánchez V, Kuba MG, Rinehart C, Arteaga CL. (2012)
Feedback upregulation of HER3 (ErbB3) expression and activity attenuates antitumor effect of PI3K inhibitors.
Proc Natl Acad Sci USA, 109 (8): 2718-23. [PMID:21368164]
2. Shapiro GI, Rodon J, Bedell C, Kwak EL, Baselga J, Braña I, Pandya SS, Scheffold C, Laird AD, Nguyen LT et al.. (2014)
Phase I safety, pharmacokinetic, and pharmacodynamic study of SAR245408 (XL147), an oral pan-class I PI3K inhibitor, in patients with advanced solid tumors.
Clin Cancer Res, 20 (1): 233-45. [PMID:24166903]
3. Wu P, Hu Y. (2012)
Small molecules targeting phosphoinositide 3-kinases.
Medchemcomm, 3 (11): 1337-1355. DOI: 10.1039/C2MD20044A