uzansertib   Click here for help

GtoPdb Ligand ID: 10626

Synonyms: INCB-053914 | INCB053914
Compound class: Synthetic organic
Comment: Uzansertib (INCB053914) is a pan-PIM kinase inhibitor that was developed by Incyte Corporation as a novel anticancer agent [1]. The chemical structure that was submitted to the WHO for the INN uzansertib is identical to the structure of INCB053914. INCB053914 is a Type 1, ATP-competitive inhibitor. The PIMs (PIM1, PIM2, and PIM3) are serine/threonine protein kinases that are important players in JAK/STAT and PI3K/AKT signalling pathways and in tumourigenesis. PIMs are known to be overexpressed in haematologic and solid tumours, and consequently PIM inhibitors are being developed and investigated for clinical anti-tumour potential.
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 8
Hydrogen bond donors 4
Rotatable bonds 5
Topological polar surface area 124.6
Molecular weight 513.2
XLogP 2.47
No. Lipinski's rules broken 0
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Canonical SMILES CC1CN(CC(C1O)N)c1c(cnc2c1CCC2O)NC(=O)c1ccc(c(n1)c1c(F)cccc1F)F
Isomeric SMILES C[C@@H]1CN(C[C@@H]([C@H]1O)N)c1c(cnc2c1CC[C@@H]2O)NC(=O)c1ccc(c(n1)c1c(F)cccc1F)F
InChI InChI=1S/C26H26F3N5O3/c1-12-10-34(11-17(30)25(12)36)24-13-5-8-20(35)22(13)31-9-19(24)33-26(37)18-7-6-16(29)23(32-18)21-14(27)3-2-4-15(21)28/h2-4,6-7,9,12,17,20,25,35-36H,5,8,10-11,30H2,1H3,(H,33,37)/t12-,17+,20+,25+/m1/s1
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Summary of Clinical Use Click here for help
INCB053914 has progressed to Phase 1/2 clinical evaluation in solid tumours (NCT02587598) and in myelodysplastic/myeloproliferative neoplasms (NCT04061421). In both of these trials INCB053914 is being tested in combination with other chemotherapy drugs.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT02587598 Study of INCB053914 in Subjects With Advanced Malignancies Phase 1/Phase 2 Interventional Incyte Corporation
NCT04061421 A Basket Study of Novel Therapy for Untreated MDS/MPN and Relapsed/Refractory Overlap Syndromes (ABNL-MARRO) Phase 1/Phase 2 Interventional Vanderbilt-Ingram Cancer Center