PLK1-IN-12
PLK1-IN-12 is a highly selective and orally active PLK1 inhibitor with an IC50 of 20 nM. PLK1-IN-12 shows more selective for PLK1 than PLK2 (IC50: >10000 nM) and PLK3 (IC50: 3953 nM). PLK1-IN-12 exhibits anticancer potency across a broad spectrum of cell lines. PLK1-IN-12 can be used in anti-leukemia research.
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。
- 分子式: C28H40ClN7O3
- 分子量:558.12
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
PLK1 20 nM (IC50) |
PLK2 >10000 nM (IC50) |
PLK3 3953 nM (IC50) |
体外実験
PLK1-IN-12 (Compound B31) (0.508 nM-10 μM, 24 h) shows antiproliferative effects in H460 (IC50: 12 nM), A549 (IC50: 32 nM), SW620 (IC50: 8.2 nM), HL-60 (IC50: 59 nM), K562 (IC50: 0.08 nM) and CCRF-CEM (IC50: 41 nM) cell lines[1].
PLK1-IN-12 (1 μM, 5 min) shows rapid clearance in human, mouse and dog liver microsomes (Clint: 68.3-210 μL/min/mg protein)[1].
PLK1-IN-12 (0.1-30 μM, 24 h) has a low inhibitory effect on HEK293T cells viability (68%)[1].
PLK1-IN-12 (0.4-100 μM) has a low inhibitory effect on hERG potassium channels (IC50: 44.2 μM), indicating a low risk of cardiotoxicity[1].
PLK1-IN-12 (10 μM, 5-30 min) has no inhibitory effect on CYP1A2, CYP3A4, CYP2D6, CYP2B6 and CYP2C8, and only has weak inhibitory effects on CYP2C9 and CYP2C19, indicating that it is stable in both human and rat hepatocytes and has a low possibility of drug interactions[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H460、PC-9、A549、SW620、HL-60、K562、CCRF-CEM and KG-1 cell lines
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Concentration:1.00 × 10-5, 3.33 × 10-6, 1.11 × 10-6, 3.7 × 10-7, 1.23 × 10-7, 4.12 × 10-8, 1.37 × 10-8, 4.57 × 10-9, 1.52 × 10-9, and 5.08 × 10-10 mol/L
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Incubation Time:24 h
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Result:Showed antiproliferative effects in H460 (IC50: 12 nM), A549 (IC50: 32 nM), SW620 (IC50: 8.2 nM), HL-60 (IC50: 59 nM), K562 (IC50: 0.08 nM) and CCRF-CEM (IC50: 41 nM) cell lines.
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Cell Line:HEK293T cells
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Concentration:0.1, 0.3, 1, 3, 10, and 30 μM
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Incubation Time:24 h
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Result:Had a low inhibitory effect on cell viability of HEK293T cells (68%).
Parmacokinetics
体内実験
PLK1-IN-12 (500 mg/kg, i.g., once daily for 7 d) has no tissue damage or toxicity to various organs of mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Subcutaneous K562 cell transplantation tumor model, Male BALB/c mice (6–8 weeks old, weighing 18–20 g)[1]
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Dosage:10/20 mg/kg
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Administration:Intragastric (i.g.), twice weekly for 11 d
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Result:Inhibited tumor growth.
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Animal Model:Acute toxicity test[1]
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Dosage:500 mg/kg
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Administration:Intragastric (i.g.), once daily for 7 d
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Result:Compared with the mice in the positive control group, there was no significant change in body weight, and no obvious damage to the heart, kidney, lung, liver and spleen.
化学情報
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分子量 558.12
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分子式 C28H40ClN7O3
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SMILES
CN(C1=O)C(C=NC(NC2=C(C(Cl)=CC(N3CCN(CC3)C)=C2)OCCCO)=N4)=C4N([C@@H]1CC)C5CCCC5
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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)
PLK1-IN-12 関連分類
HY-172364 関連分類
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