CZY43
CZY43 is a HER3 degrader with a DC50 of 559 nM. CZY43 induces HER3 degradation via autophagy, inhibits HER3-dependent signaling pathways, suppresses downstream PI3K/Akt signaling, and thereby inhibits tumor cell proliferation and cell adhesion. CZY43 can be used in studies of breast cancer and non-small cell lung cancer.
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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: C42H53Cl2N5O3
- 分子量:746.81
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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
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- 純度とドキュメンテーション
- 参考文献
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生物活性
製品説明
IC50 & Target
[1]|
HER3 559 nM (DC50) |
Akt |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SK-BR-3 | IC50 |
0.53 μM
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Antiproliferative activity against breast cancer SKBR3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay.
Antiproliferative activity against breast cancer SKBR3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay.
|
39818014 |
体外実験
CZY43 (0-2000 nM; 0-24 h) induces dose- and time-dependent degradation of HER3 in breast cancer SKBR3 cells, and effectively reduces HER3 protein levels in breast cancer MDA-MB-453 cells and non-small cell lung cancer A549 cells[1].
CZY43 (125 nM-2000 nM; 8 h) potently inhibits the HER3-dependent signaling pathway in breast cancer SKBR3 cells by reducing the protein levels of HER3 and phosphorylated AKT in a dose-dependent manner[1].
CZY43 potently inhibits the proliferation of breast cancer SKBR3 cells with an IC50 of 0.53 μM, and reduces the adhesion capacity of SKBR3 cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:breast cancer SKBR3 cells
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Concentration:1 μM; 3 μM
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Incubation Time:8 h
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Result:Degraded HER3 by 67 % at 1 μM after 8 h.
Degraded HER3 by 96 % at 3 μM after 8 h.
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Cell Line:breast cancer SKBR3 cells, breast cancer MDA-MB-453 cells, non-small cell lung cancer A549 cells
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Concentration:0, 125, 250, 500, 1000, 2000 nM (dose-dependent)
1000 nM (time-dependent) -
Incubation Time:8 h (dose-dependent)
0, 2, 4, 8, 12, 24 h (time-dependent) -
Result:Induced dose-dependent HER3 degradation in SKBR3 cells over 8 h.
Induced time-dependent HER3 degradation in SKBR3 cells across multiple timepoints.
Effectively reduced HER3 protein levels in MDA-MB-453 and A549 cells.
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Cell Line:breast cancer SKBR3 cells
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Concentration:125 nM, 250 nM, 500 nM, 1000 nM, 2000 nM
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Incubation Time:8 h
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Result:Dose-dependently reduced HER3 and p-AKT protein levels in SKBR3 cells, with more potent inhibition than bosutinib.
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Breast Cancer Modeling
- Cell Viability Determination by MTT Colorimetric Assay
- 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
- Autophagy
- Lysosome and acidic-vesicle live-cell staining
- MTT Cell Proliferation Assay
- Macroautophagy Solutions
化学情報
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分子量 746.81
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分子式 C42H53Cl2N5O3
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SMILES
COC1=CC(NC2=C(C=NC3=C2C=C(C(OCCCN4CCC5(CCN(CC5)CCC6(C7)C[C@@H]8C[C@@H](C[C@H]7C8)C6)CC4)=C3)OC)C#N)=C(C=C1Cl)Cl
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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)
CZY43 関連分類
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