APE1-IN-2
Based on 1 Customer Validation
APE1-IN-2 (compound AP1) is a Pt(IV) proagent, targeting a critical BER protein, apurinic/apyrimidinic endonuclease 1 (APE1). APE1-IN-2 shows anticancer activity. APE1-IN-2 induces intracellular accumulation of platinum and activates DNA damage response and apoptosis signals.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 98.28%
- CAS 番号: 2923433-95-6
- 分子式: C9H12Cl2N4O5Pt
- 分子量:522.21
-
保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
製品説明
体外実験
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 IC50 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
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 IC50 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 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 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.
-
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 IC50 value of 45.14 ± 17.37 μM.
体内実験
MedChemExpress (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.
化学情報
-
CAS 番号 2923433-95-6
-
性状 Solid
-
分子量 522.21
-
分子式 C9H12Cl2N4O5Pt
-
Color Light yellow to yellow
-
SMILES
O[Pt](Cl)(Cl)(OC(C1=CC2=CC=CC([N+]([O-])=O)=C2N1)=O)([NH3])[NH3]
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
純度とドキュメンテーション
-
データシート (278 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
APE1-IN-2 関連分類
HY-151883 関連分類
Powered by Bioz