CFI-400945   Click here for help

GtoPdb Ligand ID: 8063

Synonyms: CFI 400945 | CFI400945
Compound class: Synthetic organic
Comment: CFI-400945 is first-in-class oral, and selective inhibitor of polo-like kinase 4 (PLK4) [1-2]. It has advanced to clinical evaluation in selected cancer patients.
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 5
Hydrogen bond donors 2
Rotatable bonds 6
Topological polar surface area 79.48
Molecular weight 534.26
XLogP 5.19
No. Lipinski's rules broken 1
SMILES / InChI / InChIKey
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Canonical SMILES COc1ccc2c(c1)C1(CC1c1ccc3c(c1)[nH]nc3C=Cc1ccc(cc1)CN1CC(C)OC(C1)C)C(=O)N2
Isomeric SMILES COc1ccc2c(c1)[C@]1(CC1c1ccc3c(c1)[nH]nc3/C=C/c1ccc(cc1)CN1C[C@H](C)O[C@@H](C1)C)C(=O)N2
InChI InChI=1S/C33H34N4O3/c1-20-17-37(18-21(2)40-20)19-23-6-4-22(5-7-23)8-12-29-26-11-9-24(14-31(26)36-35-29)28-16-33(28)27-15-25(39-3)10-13-30(27)34-32(33)38/h4-15,20-21,28H,16-19H2,1-3H3,(H,34,38)(H,35,36)/b12-8+/t20-,21+,28?,33-/m0/s1
InChI Key DADASRPKWOGKCU-IHKPOXLFSA-N
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Summary of Clinical Use Click here for help
CFI-400945 has progressed to clinical evaluation in patients with advanced solid tumours and haematological cancers.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
PLK4 regulates centriole duplication and so is essential for cell division and proliferation. Inhibition of PLK4 has anti-proliferative action.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT01954316 A Study of CFI-400945 Fumarate in Patients With Advanced Cancer Phase 1 Interventional University Health Network, Toronto CFI-400945 (64 mg) was well tolerated in patients with advanced solid tumours. Dose-limiting toxicities (e.g. neutropenia) were observed above 64 mg. 3
NCT04176848 CFI-400945 and Durvalumab in Patients With Advanced Triple Negative Breast Cancer Phase 2 Interventional Canadian Cancer Trials Group
NCT03624543 CFI-400945 in Patients With Advanced/Metastatic Breast Cancer Phase 2 Interventional Canadian Cancer Trials Group
NCT03187288 Study of CFI-400945 Fumarate in Patients With Relapsed or Refractory AML or MDS Phase 1 Interventional University Health Network, Toronto
NCT03385655 Prostate Cancer Biomarker Enrichment and Treatment Selection Phase 2 Interventional Canadian Cancer Trials Group