Apcin

Catalog No.S9605 Batch:S960501

Technical Data

Formula

C₁₃H₁₄Cl₃N₇O₄

Molecular Weight

438.65

CAS No.

300815-04-7

Solubility (25°C)*

In vitro

DMSO

88 mg/mL (200.61 mM)

Ethanol

10 mg/mL (22.79 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	4.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil	6.6mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 132 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Apcin (APC inhibitor) is an inhibitor of the E3 ligase activity of the mitotic anaphase-promoting complex/cyclosome (APC/C) that binds to Cdc20 and competitively inhibits the ubiquitylation of D-box-containing substrates.

Targets

APC/C ^[1]

CDC20 ^[1]

In vitro

Apcin is a novel cell‑permeable molecule that blocks the interaction between APC/C and Cdc20. Apcin is demonstrated to inhibit OS cell growth and induce significant apoptosis. The invasion and mobile abilities of OS cells are also markedly suppressed by apcin treatment. Furthermore, Bim and p21 are upregulated in OS cells following apcin treatment.^[2] The inhibition of CDC20 with its inhibitor Apcin reduces the adhesion rate and proliferation ability to RL95-2 and HEC-1A cells, respectively.^[3]

In vivo

CDC20 inhibitor Apcin inhibits embryo implantation in vivo.^[3]

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines Human osteosarcoma cell lines MG63 and U2OS Concentrations 25 μM, 50 μM, 75 μM Incubation Time 24 h, 48 h, 72 h Method MG63 and U2OS (2.5×10³ cells/well) are seeded in 96‑well plates and cultured overnight. Different concentrations of apcin are added to the medium and cultured for 24, 48 and 72 h, respectively. An MTT assay is then carried out to assess the cell viability according to the manufacturer's protocols. Then, 10 μl of MTT solution (0.5 mg/ml) is added to each well followed by incubation for 4 h. The liquid supernatant is then drained off and 100 μl of DMSO is added to each well to dissolve the crystals. The absorbance of each well at 490 nm is determined using a Multimode Reader of SpectraMax M5.
Animal Study:^{^[3]}	Animal Models 8-week-old adult C57BL/6 female mice (weighing 20 to 25 g), 12-week-old adult C57BL/6 male mice (weighing 40 to 50 g) Dosages -- Administration Uterine horn injection

Cell Assay:^{^[2]}

Cell lines
Human osteosarcoma cell lines MG63 and U2OS
Concentrations
25 μM, 50 μM, 75 μM
Incubation Time
24 h, 48 h, 72 h
Method
MG63 and U2OS (2.5×10³ cells/well) are seeded in 96‑well plates and cultured overnight. Different concentrations of apcin are added to the medium and cultured for 24, 48 and 72 h, respectively. An MTT assay is then carried out to assess the cell viability according to the manufacturer's protocols. Then, 10 μl of MTT solution (0.5 mg/ml) is added to each well followed by incubation for 4 h. The liquid supernatant is then drained off and 100 μl of DMSO is added to each well to dissolve the crystals. The absorbance of each well at 490 nm is determined using a Multimode Reader of SpectraMax M5.

Animal Study:^{^[3]}

Animal Models
8-week-old adult C57BL/6 female mice (weighing 20 to 25 g), 12-week-old adult C57BL/6 male mice (weighing 40 to 50 g)
Dosages
--
Administration
Uterine horn injection

References

Selleck's Apcin has been cited by 3 publications

p53 directly downregulates the expression of CDC20 to exert anti-tumor activity in mantle cell lymphoma [ Exp Hematol Oncol, 2023, 12(1):28]	PubMed: 36882855
Inhibition of Cdc20 suppresses the metastasis in triple negative breast cancer (TNBC) [ Breast Cancer, 2021, 10.1007/s12282-021-01242-z]	PubMed: 33813687
Androgen receptor negatively regulates mitotic checkpoint signaling to induce docetaxel resistance in castration-resistant prostate cancer [ Prostate, 2021, 10.1002/pros.24257]	PubMed: 34672379

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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