Drug Information

Drug General Information
Drug ID
D09JGK
Former ID
DNCL002185
Drug Name
TAK-960
Drug Type
Small molecular drug
Indication Solid tumours [ICD9: 140-199, 210-229; ICD10:C00-D48] Phase 1 [523131]
Company
Millennium Pharmaceuticals
Structure
Download
2D MOL

3D MOL
Formula
C27H34F3N7O3
Canonical SMILES
CN1CCC(CC1)NC(=O)C2=CC(=C(C=C2F)NC3=NC=C4C(=N3)N(CC(C(=<br />O)N4C)(F)F)C5CCCC5)OC
InChI
1S/C27H34F3N7O3/c1-35-10-8-16(9-11-35)32-24(38)18-12-22(40-3)20(13-19(18)28)33-26-31-14-21-23(34-26)37(17-6-4-5-7-17)15-27(29,30)25(39)36(21)2/h12-14,16-17H,4-11,15H2,1-3H3,(H,32,38)(H,31,33,34)
InChIKey
GWRSATNRNFYMDI-UHFFFAOYSA-N
PubChem Compound ID
53357478
PubChem Substance ID
125259587, 136340376, 136345880, 137996944, 152159577, 162011971, 163370591, 170502848, 172919611, 174517180, 175448044, 185997027, 224329295, 227757866, 243109891, 249734679, 250184674, 251910552, 252155315, 252451530, 252473558, 252810940
Target and Pathway
Target(s) Serine/threonine-protein kinase PLK1 Target Info Modulator [531743]
KEGG Pathway FoxO signaling pathway
Cell cycle
Oocyte meiosis
Progesterone-mediated oocyte maturation
Pathway Interaction Database p73 transcription factor network
ATR signaling pathway
PLK1 signaling events
FoxO family signaling
FOXM1 transcription factor network
Validated transcriptional targets of TAp63 isoforms
Polo-like kinase signaling events in the cell cycle
Reactome Polo-like kinase mediated events
Golgi Cisternae Pericentriolar Stack Reorganization
APC/C:Cdh1 mediated degradation of Cdc20 and other APC/C:Cdh1 targeted proteins in late mitosis/early G1
Phosphorylation of the APC/C
Phosphorylation of Emi1
Condensation of Prophase Chromosomes
Separation of Sister Chromatids
Resolution of Sister Chromatid Cohesion
Regulation of PLK1 Activity at G2/M Transition
Activation of NIMA Kinases NEK9, NEK6, NEK7
Loss of Nlp from mitotic centrosomes
Recruitment of mitotic centrosome proteins and complexes
Loss of proteins required for interphase microtubule organization?from the centrosome
Anchoring of the basal body to the plasma membrane
RHO GTPases Activate Formins
Mitotic Prometaphase
Cyclin A/B1 associated events during G2/M transition
WikiPathways Mitotic Telophase/Cytokinesis
Mitotic Metaphase and Anaphase
Mitotic Prophase
Mitotic Prometaphase
Integrated Pancreatic Cancer Pathway
TNF alpha Signaling Pathway
Prostate Cancer
miR-targeted genes in muscle cell - TarBase
miR-targeted genes in lymphocytes - TarBase
miR-targeted genes in epithelium - TarBase
Integrated Breast Cancer Pathway
Integrated Cancer pathway
Mitotic G2-G2/M phases
Cell Cycle
APC/C-mediated degradation of cell cycle proteins
Regulation of toll-like receptor signaling pathway
References
Ref 523131ClinicalTrials.gov (NCT01179399) Study of Orally Administered TAK-960 in Patients With Advanced Nonhematologic Malignancies. U.S. National Institutes of Health.
Ref 531743TAK-960, a novel, orally available, selective inhibitor of polo-like kinase 1, shows broad-spectrum preclinical antitumor activity in multiple dosing regimens. Mol Cancer Ther. 2012 Mar;11(3):700-9.

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