[CAS NO. 2923433-95-6] APE1-IN-2
PRODUCTS SPECIFICATIONS [2923433-95-6]
DESCRIPTION [2923433-95-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 522.21 |
| Molecular Formula | C9H12Cl2N4O5Pt |
| SMILES | O[Pt](Cl)(Cl)(OC(C1=CC2=CC=CC([N+]([O-])=O)=C2N1)=O)([NH3])[NH3] |
Summary
In Vitro
APE1-IN-2 (compound AP1) can strongly inhibit the growth of malignant cells, including Cisplatin-resistant cancer cells, with up to 18.11 times inhibition compared with
Cisplatin
(HY-17394)
[1]
.
APE1-IN-2 (500 nM, 24 h) arrests the cell cycle in A549 and MCF7 cells
[1]
.
APE1-IN-2 (10 μM, 24 h) induces p53-dependent apoptosis in A549 cells
[1]
.
APE1-IN-2 (0-250 μM, 72 h) inhibits AP-cutting activity with an IC
50
of 45.14 ± 17.37 μM
[1]
.
APE1-IN-2 can directly inhibit the AP endonuclease activity of APE1, leading to an interruption of miRNA processing and upregulation of the tumor suppressor PTEN
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay [1]
| Cell Line: | A549 (non-small cell lung cancer), MCF7 (breast cancer), U251 (glioblastoma), A375 (melanoma), PC3 (prostate cancer), and HEP-G2 (hepatocarcinoma) cell lines |
| Concentration: | |
| Incubation Time: | 72 h |
| Result: | Demonstrated more potent antiproliferation effects than Cisplatin (HY-17394), with IC 50 of 0.45 ± 0.03, 0.43 ± 0.03, 4.70 ± 0.14, 0.39 ± 0.03, 5.65 ± 0.21, and 3.53 ± 0.31 μM in A549, MCF7, U251, A375, PC3, and HEP-G2 cell lines, respectively. |
Cell Cycle Analysis [1]
| Cell Line: | A549 and MCF7 cells |
| Concentration: | 500 nM |
| Incubation Time: | 24 h |
| Result: | Induced the most severe S-phase arrest in A549 and MCF7 cells. |
Cell Proliferation Assay [1]
| Cell Line: | A549 cells |
| Concentration: | 10 μM |
| Incubation Time: | 24 h |
| Result: | Caused apoptosis in approximately 38.7% (22.9% early apoptosis and 15.8% late apoptosis) of cancer cells. |
Western Blot Analysis [1]
| Cell Line: | A549 and HEK-293T cell lines |
| Concentration: | 0, 16, 40, 100, 250 μM |
| Incubation Time: | 72 h |
| Result: | Significantly increased the level of p53 by 2.09 ± 0.51-fold. Slightly raised the levels of p53, γH2A.X, and cl.PARP in HEK-293T. Inhibited AP-cutting activity with an IC 50 value of 45.14 ± 17.37 μM. |
In Vivo
APE1-IN-2 (compound AP1) (2 mg/kg, IP, once every 3 days for 15 days) exhibits an antitumor effect on the A549 xenograft model [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | BALB/c nude mice (5 week-old, female, 16 ± 2 g of body weight bearing A549 xenograft tumors) [1] |
| Dosage: | 2 mg/kg |
| Administration: | IP, once every 3 days for 15 days |
| Result: | Exhibited a 3.86-fold xenograft tumor inhibitory activity compared to Cisplatin. Did not significantly alter the body weight of mice, improving its sufficient safety. |
Shipping
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.