PKI-166
Based on 1 publication(s) in Google Scholar
PKI-166 is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM.
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。
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- 純度: 98.92%
- CAS 番号: 187724-61-4
- 分子式: C20H18N4O
- 分子量:330.38
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 PKI-166
MoreEGFR 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
IC50: 0.7 nM (EGFR tyrosine kinase)[1]
Pretreatment with PKI-166 (0-0.5 μM; 1 hour) inhibits EGFR autophosphorylation in human pancreatic cancer cells[1].
PKI-166 (0.03μ M; 6 days) enhanced the cytotoxicity mediated by gemcitabine[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:L3.6pl cells
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Concentration:0.01 μM, 0.05 μM, 0.5 μM
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Incubation Time:1 hour
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Result:Inhibited EGFR autophosphorylation in a dose-dependent manner.
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Cell Line:L3.6pl cells
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Concentration:0.03 μM
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Incubation Time:6 days
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Result:Enhanced the cytotoxicity mediated by gemcitabine.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male athymic nude mice with L3.6pl cells xenograft (8–12 weeks)[1]
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Dosage:100 mg/kg
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Administration:Oral administration; daily; from day 7 to day 35 after xenograft
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Result:Significantly decreased median tumor volume.
化学情報
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CAS 番号 187724-61-4
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性状 Solid
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分子量 330.38
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分子式 C20H18N4O
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Color White to light yellow
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SMILES
OC1=CC=C(C2=CC3=C(N=CN=C3N2)N[C@@H](C4=CC=CC=C4)C)C=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618
溶剤 & 溶解度
DMSO : ≥ 125 mg/mL (378.35 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (275 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0268 mL | 15.1341 mL | 30.2682 mL | 75.6704 mL |
| 5 mM | 0.6054 mL | 3.0268 mL | 6.0536 mL | 15.1341 mL | |
| 10 mM | 0.3027 mL | 1.5134 mL | 3.0268 mL | 7.5670 mL | |
| 15 mM | 0.2018 mL | 1.0089 mL | 2.0179 mL | 5.0447 mL | |
| 20 mM | 0.1513 mL | 0.7567 mL | 1.5134 mL | 3.7835 mL | |
| 25 mM | 0.1211 mL | 0.6054 mL | 1.2107 mL | 3.0268 mL | |
| 30 mM | 0.1009 mL | 0.5045 mL | 1.0089 mL | 2.5223 mL | |
| 40 mM | 0.0757 mL | 0.3784 mL | 0.7567 mL | 1.8918 mL | |
| 50 mM | 0.0605 mL | 0.3027 mL | 0.6054 mL | 1.5134 mL | |
| 60 mM | 0.0504 mL | 0.2522 mL | 0.5045 mL | 1.2612 mL | |
| 80 mM | 0.0378 mL | 0.1892 mL | 0.3784 mL | 0.9459 mL | |
| 100 mM | 0.0303 mL | 0.1513 mL | 0.3027 mL | 0.7567 mL |
PKI-166 関連分類
HY-117155 関連分類
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