FGFR-IN-27
FGFR-IN-27 is an orally active, broad-spectrum FGFR inhibitor, with an IC50 of 0.24 nM against human FGFR1, 0.71 nM against FGFR2, 0.87 nM against FGFR3, and 6.50 nM against FGFR4. FGFR-IN-27 inhibits cancer cell proliferation and blocks tumor growth. FGFR-IN-27 reduces the phosphorylation levels of AKT and ERK, induces apoptosis and ferroptosis, increases ROS levels, and decreases GSH levels. FGFR-IN-27 can be used in the research of 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。
- 分子式: C28H32Cl2N6O3
- 分子量:571.50
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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
- プロトコル
- 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]|
FGFR1 0.24 nM (IC50) |
FGFR2 0.71 nM (IC50) |
FGFR3 0.87 nM (IC50) |
FGFR4 6.5 nM (IC50) |
体外実験
FGFR-IN-27 (Compound 1a) (0.1 nM-10000 nM; 3 days) inhibits the proliferation of human Huh7, MHCC97-H, HepG2, MCF7 and MDA-MB-231 cells, with IC50 values of 11.0 nM, 91.2 nM, 485 nM, 4430 nM and 3380 nM, respectively[1].
FGFR-IN-2 inhibits migration and proliferation of human Huh7 hepatocellular carcinoma cells[1].
FGFR-IN-27 (0.01-10 μM) inhibits the downstream signaling pathway of FGFR in human Huh7 hepatocellular carcinoma cells by dose-dependently reducing the phosphorylation levels of AKT and ERK[1].
FGFR-IN-27 (10-100 nM; 24 h) induces apoptosis in human Huh7 hepatocellular carcinoma cells[1].
FGFR-IN-27 (0.1 μM) induces ferroptosis in human Huh7 hepatocellular carcinoma cells, increases ROS levels, and decreases glutathione (GSH) levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human hepatocellular carcinoma Huh7, MHCC97-H, HepG2 cells; human breast cancer MCF7, MDA-MB-231 cells
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Concentration:0.1, 1, 10, 100, 1000, 10000 nM
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Incubation Time:3 days
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Result:Inhibited proliferation of Huh7 cells with an IC50 of 11.0 nM.
Inhibited proliferation of MHCC97-H cells with an IC50 of 91.2 nM.
Inhibited proliferation of HepG2 cells with an IC50 of 485 nM.
Inhibited proliferation of MCF7 cells with an IC50 of 4430 nM.
Inhibited proliferation of MDA-MB-231 cells with an IC50 of 3380 nM.
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Cell Line:human hepatocellular carcinoma Huh7 cells
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Concentration:10, 50, 100 nM
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Incubation Time:24 h
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Result:Induced apoptosis in Huh7 cells significantly at 10 nM.
Induced apoptosis in Huh7 cells significantly at 50 nM.
Induced apoptosis in Huh7 cells significantly at 100 nM.
Increased apoptosis rates of Huh7 cells with higher concentrations.
Parmacokinetics
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 8 weeks old)[1]
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Dosage:10 mg/kg; 50 mg/kg
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Administration:p.o.; daily; 15 days
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Result:Achieved a 54.5% tumor growth inhibition (TGI) rate.
Achieved a 90.5% TGI rate, nearly completely suppressing tumor growth.
Caused no significant mouse weight loss throughout the study.
Showed no significant toxicity in major organs (lung, liver, spleen, kidney, heart) via hematoxylin and eosin (HE) staining at therapeutic doses.
- Somatic Cell Culture
- Liver Cancer Modeling
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Apoptosis Solutions
- Ferroptosis Solutions
- MTT Cell Proliferation Assay
- Western Blot
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- ROS/oxidative-stress fluorescent staining
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- Patient-Derived Orthotopic Xenograft (PDOX)
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- Kinase activity and phosphorylation assays
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Patient-Derived Xenograft (PDX)
- Protocol for Kinase activity and phosphorylation assays
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
化学情報
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分子量 571.50
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分子式 C28H32Cl2N6O3
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SMILES
CCN1CCN(CC1)C2=CC=C(C=C2)NC3=CC4=C(CN(C(N4C)=O)C5=C(C(OC)=CC(OC)=C5Cl)Cl)C=N3
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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)
FGFR-IN-27 関連分類
HY-183780 関連分類
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