SH-CER-6
SH-CER-6 is a double-warhead C2-COUPL derived from Ceritinib (HY-187801) that targets the EML4-ALK fusion protein complex and induces its degradation. SH-CER-6 simultaneously binds to structures near the ALK inhibitor-binding region and forms a covalent conjugate with a protein cysteine, thereby promoting ubiquitination and proteasome-dependent degradation of the EML4-ALK complex, which in turn inhibits the ALK signaling pathway. SH-CER-6 is useful for research related to ALK-positive non-small cell lung cancer.
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- Formule: C44H51ClN8O7S
- Masse moléculaire:871.44
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
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Help & FAQs
Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| NCI-H3122 | DC50 |
20 nM
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Proteasome-mediated, ubiquitin-dependent degradation of EML4-ALK fusion protein in human NCI-H3122 non-small cell lung cancer cells.
Proteasome-mediated, ubiquitin-dependent degradation of EML4-ALK fusion protein in human NCI-H3122 non-small cell lung cancer cells.
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42506886 |
In Vitro
SH-CER-6 (20 nM) induces proteasome-mediated, ubiquitin-dependent degradation of EML4-ALK in NCI-H3122 non-small cell lung cancer cells with a DC50 of 20 nM[1].
SH-CER-6 mediates cysteine-dependent degradation of EML4-ALK in multiple ALK-positive non-small cell lung cancer cell lines[1].
SH-CER-6 shows ALK-dependent toxicity comparable to parental ceritinib in a panel of non-small cell lung cancer cell lines, with dual warheads improving potency relative to a non-covalent analog[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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Masse moléculaire 871.44
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Formule C44H51ClN8O7S
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SMILES
ClC(C(NC1=CC=CC=C1S(C(C)C)(=O)=O)=N2)=CN=C2NC3=CC(C)=C(C=C3OC(C)C)C4CCN(C(CCNC(C5=CC(NC(C=C)=O)=CC(NC(C=C)=O)=C5)=O)=O)CC4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Immunoprecipitation
Immunoprecipitation (IP) is an experimental method that uses the principle of antibody specific binding to purify and enrich target proteins.
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Co-Immunoprecipitation
Co-immunoprecipitation technology can verify protein interaction based on the specific immune reaction between antibodies and antigens.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SH-CER-6 Related Classifications
HY-187801 Related Classifications
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