RO3280 is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM.
Ro3280 细胞实验
Cell Line
Concentration
Treated Time
Description
References
NB4
74 nM
24 hours
RO3280 inhibits leukemia cell proliferation with IC50 of 74 nM
Int J Mol Sci. 2015 Jan 7;16(1):1266-92.
HL60
175 nM
24 hours
RO3280 inhibits leukemia cell proliferation with IC50 of 175 nM
Int J Mol Sci. 2015 Jan 7;16(1):1266-92.
U937
186 nM
24 hours
RO3280 inhibits leukemia cell proliferation with IC50 of 186 nM
Int J Mol Sci. 2015 Jan 7;16(1):1266-92.
CCRF
162 nM
24 hours
RO3280 inhibits leukemia cell proliferation with IC50 of 162 nM
Int J Mol Sci. 2015 Jan 7;16(1):1266-92.
K562
797 nM
24 hours
RO3280 inhibits leukemia cell proliferation with IC50 of 797 nM
Int J Mol Sci. 2015 Jan 7;16(1):1266-92.
MV4-11
120 nM
24 hours
RO3280 inhibits leukemia cell proliferation with IC50 of 120 nM
Int J Mol Sci. 2015 Jan 7;16(1):1266-92.
SV-HUC-1 cells
50, 100 and 200 nM
24 and 48 hrs
RO3280 had a weaker inhibitory effect on SV-HUC-1 cells, with a maximal inhibitory effect of only 37%
J Cell Mol Med. 2017 Apr;21(4):758-767.
T24 cells
50, 100 and 200 nM
24 and 48 hrs
RO3280 inhibited cell growth and cell cycle progression, increased Wee1 expression and CDC2 phosphorylation, induced mitotic catastrophe and apoptosis
J Cell Mol Med. 2017 Apr;21(4):758-767.
5637 cells
50, 100 and 200 nM
24 and 48 hrs
RO3280 inhibited cell growth and cell cycle progression, increased Wee1 expression and CDC2 phosphorylation, induced mitotic catastrophe and apoptosis
J Cell Mol Med. 2017 Apr;21(4):758-767.
NIH/3T3 cells
2 μM
To evaluate the regulatory effect of Ro3280 on CAFs phenotype, results showed that Ro3280 reversed the activation state of CAFs.
Theranostics. 2022 May 9;12(8):3911-3927.
RBE cells
15 μM
48 hours
To evaluate the antitumor effect of Ro3280 on cholangiocarcinoma cells, results showed that Ro3280 significantly inhibited cell proliferation and induced apoptosis.
Theranostics. 2022 May 9;12(8):3911-3927.
HuCCT1 cells
15 μM
48 hours
To evaluate the antitumor effect of Ro3280 on cholangiocarcinoma cells, results showed that Ro3280 significantly inhibited cell proliferation and induced apoptosis.
Theranostics. 2022 May 9;12(8):3911-3927.
NB4 cells
100-500 nM
4-12 hours
RO3280 induced autophagy in NB4 cells, increased LC3-II levels, and increased autophagosomes observed by TEM.
Oncol Rep. 2017 Mar;37(3):1419-1429.
Ro3280 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c nude mice
5637 bladder cancer xenograft model
Intraperitoneal injection
40 mg/kg
Once every 5 days for 40 days
RO3280 significantly inhibited the growth of 5637 xenografts, increased Wee1 expression and CDC2 phosphorylation, and decreased BubR1 expression
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