Pinafide
Pinafide is an orally active anticancer agent. Pinafide binds to double-stranded DNA via intercalation, stabilizes the DNA-topoisomerase II complex, induces photo-induced DNA damage and ROS production, causes lysosomal and mitochondrial dysfunction, impairs DNA and RNA synthesis, and blocks cell growth. Pinafide binds to human serum albumin in vitro, undergoes biotransformation via reduction and acetylation in rats, and can cross the placental barrier of pregnant rats. Pinafide can be used in cancer-related research such as hepatocellular carcinoma.
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。
- CAS 番号: 54824-20-3
- 分子式: C18H17N3O4
- 分子量:339.35
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
DNA/RNA Synthesis アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
1.23 μM
|
Antiproliferative activity against human hepatocellular carcinoma HepG2 cells assessed as inhibition of cell growth by MTT tetrazolium dye assay.
Antiproliferative activity against human hepatocellular carcinoma HepG2 cells assessed as inhibition of cell growth by MTT tetrazolium dye assay.
|
33803403 |
体外実験
Pinafide (10-50 μg/mL) binds to human serum albumin, with one high-affinity, low-binding-capacity site (K1 = 2.8×106 M-1) and one moderate-affinity, high-binding-capacity site (K2 = 5.3×103 M-1)[1].
Pinafide is a classic DNA intercalator that stabilizes calf thymus DNA, with a ΔTm of 6.50 °C and a binding constant of 6.60 × 104 M-1[2].
Pinafide potently inhibits the proliferation of human hepatocellular carcinoma HepG2 cells, with an IC50 value of 1.23 μM; when applied at the IC50 concentration of 1.23 μM, it induces G2/M phase cell cycle arrest in human hepatocellular carcinoma HepG2 cells[2].
Pinafide (0.615 μM; 24 h) induces reactive oxygen species production in human hepatocellular carcinoma HepG2 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
Pinafide (10 mg/kg; i.v.; single bolus) crosses the placental barrier in pregnant Sprague-Dawley rats, with fetus and amniotic fluid concentrations exceeding or matching maternal blood concentrations 1 hour after i.v. administration[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 54824-20-3
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分子量 339.35
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分子式 C18H17N3O4
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SMILES
O=C1C2=C3C(C(N1CCN4CCCC4)=O)=CC([N+]([O-])=O)=CC3=CC=C2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)