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Synonyms: compound 26h [PMID: 22148278] | SB-1317 | SB1317 | TG-02 | zotiraciclib (proposed INN)
Compound class: Synthetic organic
Comment: TG02 is an orally active multi-kinase inhibitor, with a unique activity profile against CDKs, JAK2 and FLT3 [4-5]. Like pacritinib it is a small molecule macrocycle. TG02 was rationally designed to inhibit several key signaling pathways simultaneously with the aim of maximising anti-cancer efficacy. It is being investigated for its anti-leukemic potential [2-3].
The compound is administered as the citrate salt.
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. Goh KC, Novotny-Diermayr V, Hart S, Ong LC, Loh YK, Cheong A, Tan YC, Hu C, Jayaraman R, William AD et al.. (2012)
TG02, a novel oral multi-kinase inhibitor of CDKs, JAK2 and FLT3 with potent anti-leukemic properties.
Leukemia, 26 (2): 236-43. [PMID:21860433]
2. Pallis M, Abdul-Aziz A, Burrows F, Seedhouse C, Grundy M, Russell N. (2012)
The multi-kinase inhibitor TG02 overcomes signalling activation by survival factors to deplete MCL1 and XIAP and induce cell death in primary acute myeloid leukaemia cells.
Br. J. Haematol., 159 (2): 191-203. [PMID:22934750]
3. Pallis M, Burrows F, Whittall A, Boddy N, Seedhouse C, Russell N. (2013)
Efficacy of RNA polymerase II inhibitors in targeting dormant leukaemia cells.
BMC Pharmacol Toxicol, 14: 32. [PMID:23767415]
4. Poulsen A, William A, Blanchard S, Nagaraj H, Williams M, Wang H, Lee A, Sun E, Teo EL, Tan E et al.. (2013)
Structure-based design of nitrogen-linked macrocyclic kinase inhibitors leading to the clinical candidate SB1317/TG02, a potent inhibitor of cyclin dependant kinases (CDKs), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase-3 (FLT3).
J Mol Model, 19 (1): 119-30. [PMID:22820730]
5. William AD, Lee AC, Goh KC, Blanchard S, Poulsen A, Teo EL, Nagaraj H, Lee CP, Wang H, Williams M et al.. (2012)
Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[22.214.171.124(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinase-3 (FLT3) for the treatment of cancer.
J. Med. Chem., 55 (1): 169-96. [PMID:22148278]