zotiraciclib   Click here for help

GtoPdb Ligand ID: 9095

Synonyms: compound 26h [PMID: 22148278] | SB-1317 | SB1317 | TG-02 | TG02
Compound class: Synthetic organic
Comment: Zotiraciclib (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 simultaneously inhibit several key signalling pathways, 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.
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 4
Hydrogen bond donors 1
Rotatable bonds 0
Topological polar surface area 50.28
Molecular weight 372.2
XLogP 4.29
No. Lipinski's rules broken 0
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Canonical SMILES CN1CC=CCCOc2cccc(c2)c2nc(Nc3cc(C1)ccc3)ncc2
Isomeric SMILES CN1C/C=C/CCOc2cccc(c2)c2nc(Nc3cc(C1)ccc3)ncc2
InChI InChI=1S/C23H24N4O/c1-27-13-3-2-4-14-28-21-10-6-8-19(16-21)22-11-12-24-23(26-22)25-20-9-5-7-18(15-20)17-27/h2-3,5-12,15-16H,4,13-14,17H2,1H3,(H,24,25,26)/b3-2+
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Summary of Clinical Use Click here for help
TG02 is being evaluated in Phase 1 clinical trials for chronic lymphocytic leukemia or small lymphocytic lymphoma (NCT01699152; dose ranging study) and advanced hematological malignancies (NCT01204164; dose-escalation study with arms investigating TG02 as a monotherapy, in combination with carfilzomib and dexamethasone in multiple myeloma patients and in combination with carfilzomib and dexamethasone in carfilzomib refractory multiple myeloma patients).
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT01204164 Phase 1 Study of TG02 Citrate in Patients With Advanced Hematological Malignancies Phase 1 Interventional Tragara Pharmaceuticals, Inc.
NCT01699152 Phase 1 Study of TG02 Citrate in Patients With Chronic Lymphocytic Leukemia and Small Lymphocytic Lymphoma Phase 1 Interventional Tragara Pharmaceuticals, Inc.