SH-CER-6
SH-CER-6 is a dual-warhead C2-COUPL derived from ceritinib, which targets the EML4-ALK fusion protein complex and induces its degradation. By simultaneously binding to the structure near the ALK inhibitor-binding region and forming a covalent conjugate with protein cysteines, SH-CER-6 promotes ubiquitination and proteasome-dependent degradation of the EML4-ALK complex, thereby inhibiting the ALK signaling pathway. SH-CER-6 induces EML4-ALK degradation in H3122 cells with a DC50 of 20 nM, and can be used in studies related to ALK-positive non-small cell lung cancer.
For research use only. We do not sell to patients.
- Formula: C44H51ClN8O7S
- Molecular Weight:871.44
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 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 |
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.
Chemical Information
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Molecular Weight 871.44
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SH-CER-6 Related Classifications
HY-187801 Related Classifications
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