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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- Fòrmula: C42H53Cl2N5O3
- Peso molecular:746.81
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
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.
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39818014 |
In Vitro
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
Chemical Information
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Peso molecular 746.81
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CZY43 Related Classifications
HY-172091 Related Classifications
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