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Synonyms: INK 128 | INK-128 | INK128 | MLN0128 | TAK-228
Compound class: Synthetic organic
Comment: Sapanisertib (INK128) is an ATP-competitive inhibitor of mTOR in mTORC1 and mTORC2 complexes, that exhibits potent anti-tumour activity [1-3].
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. Hsieh AC, Liu Y, Edlind MP, Ingolia NT, Janes MR, Sher A, Shi EY, Stumpf CR, Christensen C, Bonham MJ et al.. (2012)
The translational landscape of mTOR signalling steers cancer initiation and metastasis.
Nature, 485 (7396): 55-61. [PMID:22367541]
2. Jessen K, Wang S, Kessler, L, Guo X, Kucharski J, Staunton J, Lan L, Elia M, Stewart J, Brown J et al.. (2009)
INK128 is a potent and selective TORC1/2 inhibitor with broad oral anti-tumor activity.[Abstract].
Mol Cancer Ther, 8 (12 (Supplement)): B148.
3. Liu Q, Thoreen C, Wang J, Sabatini D, Gray NS. (2009)
mTOR Mediated Anti-Cancer Drug Discovery.
Drug Discov Today Ther Strateg, 6 (2): 47-55. [PMID:20622997]
4. Schenone S, Brullo C, Musumeci F, Radi M, Botta M. (2011)
ATP-competitive inhibitors of mTOR: an update.
Curr Med Chem, 18 (20): 2995-3014. [PMID:21651476]