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Chemical Structure| 1062243-51-9 Chemical Structure| 1062243-51-9
Chemical Structure| 1062243-51-9
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Product Details of Ro3280

CAS No. :1062243-51-9
Formula : C27H35F2N7O3
M.W : 543.61
SMILES Code : O=C(NC1CCN(C)CC1)C2=CC=C(NC3=NC=C(N4C)C(N(C5CCCC5)CC(F)(F)C4=O)=N3)C(OC)=C2
Synonyms :
Ro5203280
MDL No. :MFCD22665717

Safety of Ro3280

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H317-H319
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • PLK1

    PLK1, IC50:3 nM

In Vitro:

Cell Line
Concentration Treated Time Description Reference
CCRF 162 nM 24 hours RO3280 inhibits leukemia cell proliferation with IC50 of 162 nM PMC4307303
K562 797 nM 24 hours Inhibition of cell proliferation PMC4307303
NB4 74 nM 24 hours RO3280 inhibits leukemia cell proliferation with IC50 of 74 nM PMC4307303
HL60 175 nM 24 hours RO3280 inhibits leukemia cell proliferation with IC50 of 175 nM PMC4307303
U937 186 nM 24 hours RO3280 inhibits leukemia cell proliferation with IC50 of 186 nM PMC4307303
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. PMC9131280
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. PMC9131280
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. PMC9131280
MV4-11 120 nM 24 hours To evaluate the effect of PLX51107 on AML cell viability, results showed that PLX51107 reduced AML cell viability PMC4307303
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% PMC5345669
T24 cells 50, 100 and 200 nM 24 and 48 hrs Inhibited RSK4 activation, resulting in decreased cellular cIAP1 and cIAP2 expression PMC5345669
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 PMC5345669
NB4 cells 100-500 nM 4-12 hours RO3280 induced autophagy in NB4 cells, increased LC3-II levels, and increased autophagosomes observed by TEM. PMC5364848

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
FVB/N mice AKT/YapS127A-induced primary cholangiocarcinoma model Intravenous injection 6 days of administration, lasting for 21 days To evaluate the antitumor efficacy of AA-HA-ODA/Ro in vivo, results showed that AA-HA-ODA/Ro significantly inhibited tumor growth and reduced CAFs positive area. PMC9131280
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 PMC5345669

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.84mL

0.37mL

0.18mL

9.20mL

1.84mL

0.92mL

18.40mL

3.68mL

1.84mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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