PROTAC ALK degrader-5
PROTAC ALK degrader-5 (Compound 17) is an efficient ALK PROTAC degrader, with its inhibitory effects on EML4-ALK and NPM-ALK being 27.4 nM and 116.5 nM respectively. PROTAC ALK degrader-5 exhibits potent anti-proliferative activity against H3122 and Karpas 299. PROTAC ALK degrader-5 effectively inhibits the phosphorylation of ALK and STAT3. PROTAC ALK degrader-5 can be used for the study of ALK-driven malignant tumors, such as human non-small cell lung cancer and anaplastic large cell lymphoma.
(Pink: Anaplastic lymphoma kinase (ALK) Target protein ligand; Blue: Cereblon ligand (HY-14658); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 2379672-57-6
- Formula: C40H37N7O6
- Molecular Weight:711.77
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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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Biological Activity
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STAT3 |
Cereblon |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KARPAS-299 | IC50 |
42 nM
Compound: 17
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Antiproliferative activity against ALK-positive human KARPAS-299 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against ALK-positive human KARPAS-299 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
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[PMID: 34176264] |
Chemical Information
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CAS No. 2379672-57-6
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Molecular Weight 711.77
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Formula C40H37N7O6
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SMILES
O=C(N1)C(N2C(C3=CC=CC(NCC(N4CCN(C5=CC(C6(C)C)=C(C(C7=C6NC8=C7C=CC(C#N)=C8)=O)C=C5CC)CC4)=O)=C3C2=O)=O)CCC1=O
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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)
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