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Chemical Structure| 300815-04-7 Chemical Structure| 300815-04-7

Structure of Apcin
CAS No.: 300815-04-7

Chemical Structure| 300815-04-7

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Apcin is an inhibitor of the anaphase-promoting complex/cyclosome (APC/C).

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Product Details of Apcin

CAS No. :300815-04-7
Formula : C13H14Cl3N7O4
M.W : 438.65
SMILES Code : O=C(OCCN1C([N+]([O-])=O)=CN=C1C)NC(NC2=NC=CC=N2)C(Cl)(Cl)Cl
MDL No. :MFCD00525727
InChI Key :ZEXHXVOGJFGTRX-UHFFFAOYSA-N
Pubchem ID :2830389

Safety of Apcin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P302+P352-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • E3 Ligase

In Vitro:

Cell Line
Concentration Treated Time Description References
H9C2 cells 2 μM 24 h To assess the potential damage of DOX to cardiomyocytes, observed vacuolization and reduction in cell count. PMC11884132
JVM2 cells 50 μM, 100 μM, 200 μM 24h, 48h, 72h Inhibit cell proliferation, migration and invasion, induce cell apoptosis and cell cycle arrest PMC9990225
Z138 cells 50 μM, 100 μM, 200 μM 24h, 48h, 72h Inhibit cell proliferation, migration and invasion, induce cell apoptosis and cell cycle arrest PMC9990225
RPE1 cells 25 μM 45 h To evaluate the effects of apcin and proTAME on mitotic duration. Results showed that apcin and proTAME synergistically prolonged mitotic duration. PMC4214887
Cells in mitotic Xenopus egg extract 200 μM 40 min To evaluate the effects of apcin and its derivatives on the degradation of the N-terminal fragment of cyclin B1. Results showed that apcin effectively inhibited degradation. PMC4214887
HCT116 cells 50 μM 24 h To determine the effect of apcin on cyclin B1 degradation, results showed that apcin accelerated cyclin B1 degradation. PMC7289404
HTERT-RPE1 H2B-GFP cells 0, 3.1, 6.2, 12.5, 25, 50 μM 24 h To determine the effect of apcin on mitotic fraction, results showed that apcin dose-dependently decreased the mitotic fraction. PMC7289404
PC3 cells 50 µM 48 h To evaluate the effect of Apcin on PC3 cell viability and apoptosis, results showed that Apcin reduced cell viability and induced apoptosis in a dose-dependent manner PMC5148662

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J mice TRAMP-C2 subcutaneous tumor model Intraperitoneal injection 15 mg/kg Once daily ,4 days per cycle To evaluate the anti-tumor effect of Apcin combined with anti-PD1 antibodies PMC10391908
C57BL/6 mice DOX-induced myocardial injury model Intraperitoneal injection 1.5 mg/kg Once daily for 4 weeks To evaluate the effect of CDC20 inhibitor Apcin on DOX-induced myocardial injury, found that Apcin exacerbated cardiomyocyte apoptosis. PMC11884132
Balb/c nude mice Z138 cell-driven xenograft tumor model Intraperitoneal injection 20 mg/kg Every other day for 2 weeks Evaluate the anti-tumor effect and safety of Apcin in vivo PMC9990225

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.28mL

0.46mL

0.23mL

11.40mL

2.28mL

1.14mL

22.80mL

4.56mL

2.28mL

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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