Investor Presentaiton
21
Rigosertib identified as lead PLK1 inhibitor in RDEB CSCC
Inhibitor
Pharma
BI 2536
Boehringer Ingelheim,
Ingelheim, Germany
Supplier
Selleck Chemicals,
Houston, TX
PLK 1 IC 50
Clinical trial
Delivery
IC50 0.83nM
Phase II
complete
IV
GW843682X
GSK461364
GlaxoSmithKline,
Middlesex, UK
GlaxoSmithKline,
Middlesex, UK
Tocris Biosciences,
Bristol, UK
Selleck Chemicals,
Houston, TX
IC50 2.2nM
IC50 2.2nM
EC50 <100nm
in cell lines
Phase I
complete
IV
TKM-080301
Tekmira Pharmaceuticals
Corporation
Phase I
recruiting
IV
NMS-1286937
Nerviano Medical
Sciences, Milano, Italy
BI 6727
Boehringer Ingelheim,
Ingelheim, Germany
Active Biocehmical Co.,
Ltd. or Jihpharma
Shanghai Sun-shine
Chemical Technology
Co., Ltd.
Phase I
recruiting
Oral
Phase II
recruiting
IV
References
Steegmaier et al. Current
Biology.2007 17(4):316-322
Lansing et al (2007)
Mol. Cancer Ther. 6 450.
Sato Y et al. Bioorg Med Chem
Lett. 2009 19(16):4673-8.
Beria et al., Presented at
EORTC-NCI-AACR 2008;
Geneva, Switzerland.
Rudolph et al., Presented at
EORTC-NCI-AACR Geneva,
Switzerland, 2008.
CYC-800
Cyclacel Ltd, Dundee, UK
TAK-960
ON-01910
Millennium
Onconova Therapeutic,
Newtown, PA
EC50 low nM
range
Oral
AACR 2010 abstract
Phamaceuticals, C.
Selleck Chemicals,
Houston, TX
IC50 9nM
EC50 50-250nM
Phase I
Tecruiting
Phase II
recruiting
Oral
IP
Gumireddy K et al. Cancer
Cell. 2005 7(3):275-86.
OL
Kyoto, Japan
5-(5,6-Dimoxy-1H-
benzi-1-yl)-3-[[4-
(methylsulfonyl)phenyl
]methoxy]-2-T.
Houston, TX
OTAVA Ltd, Toronto,
Canada
F050 110
IC50 6.9nM
ZK-Thiazolidinone
(TAL)
Bayer
Schering Pharma AG
N/A
IC50 19nM
Cell lines EC50
0.2-1.3uM
DAP-81
Rockefeller University,
New York
IC50 0.9nM
Clin Cancer Res March 7 2019 DOI:10.1158/1078-0432.CCR-18-2661. PMID: 30846478
2003 63:6942-7
Santamaria et al (2007) Mol
Biol Cell
18, 4024-4036
Peters et al., Nat Chem Biol
2006;2:618-626.
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