PDK1 inhibitor


CAS No. : 1001409-50-2

PDK1 inhibitor,1001409-50-2
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000072
Synonyms:1-[(3,4-difluorophenyl)methyl]-2-oxo-N-[(1R)-2-[(2-oxo-1,3-dihydrobenzimidazol-5-yl)oxy]-1-phenylethyl]pyridine-3-carboxamide
Molecular Formula:C28H22F2N4O4
Molecular Weight:516.5
Target:PDK-1
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Cat No:I000072
Cas No:1001409-50-2
Product-Name:PDK1 inhibitor
IUPAC Name:1-[(3,4-difluorophenyl)methyl]-2-oxo-N-[(1R)-2-[(2-oxo-1,3-dihydrobenzimidazol-5-yl)oxy]-1-phenylethyl]pyridine-3-carboxamide
InChI:InChI=1S/C28H22F2N4O4/c29-21-10-8-17(13-22(21)30)15-34-12-4-7-20(27(34)36)26(35)31-25(18-5-2-1-3-6-18)16-38-19-9-11-23-24(14-19)33-28(37)32-23/h1-14,25H,15-16H2,(H,31,35)(H2,32,33,37)/t25-/m0/s1
InChIKey:GCWCGSPBENFEPE-VWLOTQADSA-N
SMILES:C1=CC=C(C=C1)C(COC2=CC3=C(C=C2)NC(=O)N3)NC(=O)C4=CC=CN(C4=O)CC5=CC(=C(C=C5)F)F

PDK1 inhibitor is a potent and selective inhibitor of PDK1 with potential as anticancer agent with IC50 of 1 nM, displays >3,000-fold selectivity against a panel of 256 kinases; specifically inhibits cellular PDK1 T-loop phosphorylation (Ser-241), inhibits p-RSK S221 in PC-3 cells with EC50 of 300 nM, inhibits colony formation in a subset of cancer cell lines (4 of 10) and primary xenograft tumor lines (9 of 57).

1. ACS Chem Neurosci. 2017 Jan 18;8(1):100-114. doi: 10.1021/acschemneuro.6b00251. Epub 2016 Nov 10.
Dual Inhibition of PDK1 and Aurora Kinase A: An Effective Strategy to Induce Differentiation and Apoptosis of Human Glioblastoma Multiforme Stem Cells.
Daniele S, Sestito S, Pietrobono D, Giacomelli C, Chiellini G, Di Maio D(1), Marinelli L(2), Novellino E(2), Martini C, Rapposelli S.
Author information:
(1)Scuola Normale Superiore , Piazza dei Cavalieri 7, I-56126 Pisa, Italy.
(2)Department of Pharmacy, University of Naples Federico II , Napoli, Italy.

The poor prognosis of glioblastoma multiforme (GBM) is mainly attributed to drug resistance mechanisms and to the existence of a subpopulation of glioma stem cells (GSCs). Multitarget compounds able to both affect different deregulated pathways and the GSC subpopulation could escape tumor resistance and, most importantly, eradicate the stem cell reservoir. In this respect, the simultaneous inhibition of phosphoinositide-dependent kinase-1 (PDK1) and aurora kinase A (AurA), each one playing a pivotal role in cellular survival/migration/differentiation, could represent an innovative strategy to overcome GBM resistance and recurrence. Herein, the cross-talk between these pathways was investigated, using the single-target reference compounds MP7 (PDK1 inhibitor) and Alisertib (AurA inhibitor). Furthermore, a new ligand, SA16, was identified for its ability to inhibit the PDK1 and the AurA pathways at once, thus proving to be a useful tool for the simultaneous inhibition of the two kinases. SA16 blocked GBM cell proliferation, reduced tumor invasiveness, and triggered cellular apoptosis. Most importantly, the AurA/PDK1 blocker showed an increased efficacy against GSCs, inducing their differentiation and apoptosis. To the best of our knowledge, this is the first report on combined targeting of PDK1 and AurA. This drug represents an attractive multitarget lead scaffold for the development of new potential treatments for GBM and GSCs.
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