Drug Information

Drug General Information
Drug ID
D0O0LQ
Former ID
DCL000067
Drug Name
BI 2536
Synonyms
BI2536, BI 2536
Drug Type
Small molecular drug
Indication Acute myeloid leukemia [ICD9: 205; ICD10:C92.0] Phase 2 [522354], [541009]
Therapeutic Class
Anticancer Agents
Company
Boehringer Ingelheim
Structure
Download
2D MOL

3D MOL
Formula
C28H39N7O3
InChI
InChI=1S/C28H39N7O3/c1-5-22-27(37)34(3)23-17-29-28(32-25(23)35(22)20-8-6-7-9-20)31-21-11-10-18(16-24(21)38-4)26(36)30-19-12-14-33(2)15-13-19/h10-11,16-17,19-20,22H,5-9,12-15H2,1-4H3,(H,30,36)(H,29,31,32)/t22-/m1/s1
InChIKey
XQVVPGYIWAGRNI-JOCHJYFZSA-N
CAS Number
CAS 755038-02-9
PubChem Compound ID
11364421
PubChem Substance ID
16456896, 23520952, 42443678, 47169965, 56374263, 79390480, 99436986, 103624610, 121279843, 123051122, 124757007, 125163812, 126581999, 126644897, 126671463, 126728164, 131480686, 134338770, 135263659, 135697720, 135727443, 136367307, 136368050, 136920290, 137134451, 137275913, 140810822, 143498076, 144115705, 152234950, 152258817, 152344043, 160647667, 162011967, 162037442, 162202556, 164789122, 165246686, 170494860, 172131314, 172659573, 172818898, 176223554, 177748502, 178102294, 180177875, 184826694, 186525083, 188899500, 198984127
Target and Pathway
Target(s) Serine/threonine-protein kinase PLK1 Target Info Inhibitor [536354], [537386]
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 522354ClinicalTrials.gov (NCT00701766) BI 2536 Infusional Treatment in Patients Over 60 Years of Age With Refractory or Relapsed Acute Myeloid Leukaemia. U.S. National Institutes of Health.
Ref 541009(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5666).
Ref 536354BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo. Curr Biol. 2007 Feb 20;17(4):316-22. Epub 2007 Feb 8.
Ref 537386Polo-like kinase (PLK) inhibitors in preclinical and early clinical development in oncology. Oncologist. 2009 Jun;14(6):559-70. Epub 2009 May 27.

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