KX2-361   Click here for help

GtoPdb Ligand ID: 10004

Synonyms: KX-02 | KX2 361 | KX2361
Compound class: Synthetic organic
Comment: KX2-361 is a small molecule with a dual mode of action. It is a Src kinase inhibitor and an inhibitor of tubulin polymerization [1]. It is being investigated for antiproliferative potential. It is closely related to tirbanibulin, and like KX2-391 is a peptide substrate site binder rather than a competitive ATP binding site inhibitor. KX2-361 is orally bioavailable and shows a significant level of brain tissue exposure following oral administration.
2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 5
Hydrogen bond donors 1
Rotatable bonds 7
Topological polar surface area 54.46
Molecular weight 405.19
XLogP 3.82
No. Lipinski's rules broken 0
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Canonical SMILES O=C(Cc1ccc(cn1)c1ccc(cc1)N1CCOCC1)NCc1cccc(c1)F
Isomeric SMILES O=C(Cc1ccc(cn1)c1ccc(cc1)N1CCOCC1)NCc1cccc(c1)F
InChI InChI=1S/C24H24FN3O2/c25-21-3-1-2-18(14-21)16-27-24(29)15-22-7-4-20(17-26-22)19-5-8-23(9-6-19)28-10-12-30-13-11-28/h1-9,14,17H,10-13,15-16H2,(H,27,29)
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Summary of Clinical Use Click here for help
KX2-361 is being evaluated in Phase 1 safety, tolerability and pharmacokinetics clinical trial as an antiproliferative therapy for advanced malignancies that are refractory to conventional drugs (see NCT02326441).
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT02326441 Safety, Tolerability & PK of KX2-361 in Subjects w Adv. Malignancies Refractory to Conventional Therapies Phase 1 Interventional Athenex, Inc.