tinodasertib   Click here for help

GtoPdb Ligand ID: 12385

Synonyms: AUM-001 | AUM001 | compound 48 [PMID: 29683667] | ETC-1907206 | ETC-206 | ETC206
Compound class: Synthetic organic
Comment: Tinodasertib (ETC-206) is an inhibitor of MAPK interacting serine/threonine kinases 1 and 2 [3]. It is an oncology clinical lead [1-2].
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 5
Hydrogen bond donors 0
Rotatable bonds 4
Topological polar surface area 70.63
Molecular weight 408.16
XLogP 4.45
No. Lipinski's rules broken 0
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Canonical SMILES N#Cc1ccc(cc1)c1cnc2n1cc(cc2)c1ccc(cc1)C(=O)N1CCOCC1
Isomeric SMILES C1COCCN1C(=O)c1ccc(cc1)c1cn2c(ncc2c2ccc(cc2)C#N)cc1
InChI InChI=1S/C25H20N4O2/c26-15-18-1-3-20(4-2-18)23-16-27-24-10-9-22(17-29(23)24)19-5-7-21(8-6-19)25(30)28-11-13-31-14-12-28/h1-10,16-17H,11-14H2
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Summary of Clinical Use Click here for help
A clinical trial that was designed to evaluate ETC-206's efficacy in combination with dasatinib for advanced haematologic malignancies was withdrawn. As AUM001, development is continuing in metastatic colorectal cancer.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT03414450 Evaluation of ETC-1907206 With Dasatinib in Advanced Haematologic Malignancies Phase 1 Interventional EDDC (Experimental Drug Development Centre), A*STAR Research Entities
NCT05462236 MNK Inhibitor AUM001 in Combination With Either Pembrolizumab or Irinotecan to Treat Metastatic Colorectal Cancer Phase 2 Interventional AUM Biosciences Pte Ltd