- Guide to PHARMACOLOGY
Synonyms: BEZ235 | NVP-BEZ235 | RTB-101 | RTB101
Compound class: Synthetic organic
Comment: Dactolisib is an orally bioavailable dual PI3K/mTOR inhibitor with potential antineoplastic activity. It inhibits all of the PI3K isoforms  and in addition, it effectively targets ATR with IC50 of 21 nM in cells .
COVID-19: Dactolisib (as RTB101) is being evaluated as post-exposure prophylaxis for SARS-CoV-2 infection.
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. Fròsina G, Profumo A, Marubbi D, Marcello D, Ravetti JL, Daga A. (2018)
ATR kinase inhibitors NVP-BEZ235 and AZD6738 effectively penetrate the brain after systemic administration.
Radiat Oncol, 13 (1): 76. [PMID:29685176]
2. Ma BB, Lui VW, Hui CW, Lau CP, Wong CH, Hui EP, Ng MH, Cheng SH, Tsao SW, Tsang CM et al.. (2014)
Preclinical evaluation of the mTOR-PI3K inhibitor BEZ235 in nasopharyngeal cancer models.
Cancer Lett, 343 (1): 24-32. [PMID:24041865]
3. Maira SM, Stauffer F, Brueggen J, Furet P, Schnell C, Fritsch C, Brachmann S, Chène P, De Pover A, Schoemaker K et al.. (2008)
Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity.
Mol Cancer Ther, 7 (7): 1851-63. [PMID:18606717]
4. Toledo LI, Murga M, Zur R, Soria R, Rodriguez A, Martinez S, Oyarzabal J, Pastor J, Bischoff JR, Fernandez-Capetillo O. (2011)
A cell-based screen identifies ATR inhibitors with synthetic lethal properties for cancer-associated mutations.
Nat Struct Mol Biol, 18 (6): 721-7. [PMID:21552262]
5. Willemsen-Seegers N, Uitdehaag JCM, Prinsen MBW, de Vetter JRF, de Man J, Sawa M, Kawase Y, Buijsman RC, Zaman GJR. (2017)
Compound Selectivity and Target Residence Time of Kinase Inhibitors Studied with Surface Plasmon Resonance.
J Mol Biol, 429 (4): 574-586. [PMID:28043854]