Drug Information

Drug General Information
Drug ID
D02RJY
Former ID
DCL001078
Drug Name
PHA-739358
Synonyms
Danusertib; PHA 739358; Danusertib, PHA-739358; (R)-N-(5-(2-methoxy-2-phenylacetyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)-4-(4-methylpiperazin-1-yl)benzamide; 5-Amido-pyrrolopyrazole 9d
Drug Type
Small molecular drug
Indication Prostate cancer [ICD9: 185; ICD10:C61] Phase 2 [542852], [548410]
Company
Pfizer; Nerviano
Structure
Download
2D MOL

3D MOL
Formula
C26H30N6O3
InChI
InChI=1S/C26H30N6O3/c1-30-12-14-31(15-13-30)20-10-8-19(9-11-20)25(33)27-24-21-16-32(17-22(21)28-29-24)26(34)23(35-2)18-6-4-3-5-7-18/h3-11,23H,12-17H2,1-2H3,(H2,27,28,29,33)/t23-/m1/s1
InChIKey
XKFTZKGMDDZMJI-HSZRJFAPSA-N
PubChem Compound ID
11442891
PubChem Substance ID
16541138, 23585151, 42521925, 46394298, 46513412, 57304411, 77307760, 93581266, 99373541, 99436985, 103573135, 124757005, 125163810, 126626959, 126634887, 126665979, 126730902, 131480684, 134964424, 135261930, 136340130, 136367305, 136367975, 136920406, 137147906, 137276047, 140478603, 143499036, 144115881, 152036110, 152134559, 152164575, 152186748, 152239915, 152258104, 152344035, 160646943, 162011705, 162037440, 162202553, 163109117, 164193992, 164838824, 174006483, 177748769, 180177283, 188899502, 198940281, 223682527, 223704702
Target and Pathway
Target(s) Aurora protein kinase Target Info Inhibitor [527513]
mRNA of Aurora B Target Info Inhibitor [527513]
Aurora kinase B Target Info Inhibitor [537564]
Aurora kinase A Target Info Inhibitor [537564]
KEGG Pathway Oocyte meiosishsa04114:Oocyte meiosis
Pathway Interaction Database Aurora B signaling
Signaling by Aurora kinases
Aurora C signaling
FOXM1 transcription factor network
Aurora A signalingaurora_b_pathway:Aurora B signaling
Integrin-linked kinase signaling
PLK1 signaling events
Aurora A signaling
Reactome APC/C:Cdh1 mediated degradation of Cdc20 and other APC/C:Cdh1 targeted proteins in late mitosis/early G1
Separation of Sister Chromatids
Resolution of Sister Chromatid Cohesion
RHO GTPases Activate ForminsR-HSA-174178:APC/C:Cdh1 mediated degradation of Cdc20 and other APC/C:Cdh1 targeted proteins in late mitosis/early G1
RHO GTPases Activate Formins
Mitotic PrometaphaseR-HSA-174178:APC/C:Cdh1 mediated degradation of Cdc20 and other APC/C:Cdh1 targeted proteins in late mitosis/early G1
Regulation of PLK1 Activity at G2/M Transition
WikiPathways EGF/EGFR Signaling Pathway
JAK/STAT
Gastric Cancer Network 1
Integrated Breast Cancer Pathway
APC/C-mediated degradation of cell cycle proteinsWP2757:Mitotic Metaphase and Anaphase
Mitotic Prometaphase
Regulation of Microtubule Cytoskeleton
miR-targeted genes in lymphocytes - TarBase
miR-targeted genes in epithelium - TarBase
APC/C-mediated degradation of cell cycle proteinsWP437:EGF/EGFR Signaling Pathway
APC/C-mediated degradation of cell cycle proteins
References
Ref 542852(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: 7937).
Ref 548410Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025382)
Ref 527513J Med Chem. 2005 Apr 21;48(8):3080-4.Potent and selective Aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition.
Ref 537564Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.

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