Lys-PEG3-BA
Lys-PEG3-BA is an EML4-ALK/EGFR PROTAC degrader with DC50 values of 1.32 and 19.66 μM for H3122 (EML4-ALK) and H1975 (EGFR-L858R/T790M) cells, respectively. Lys-PEG3-BA hinders proliferation via rewiring the ubiquitin- proteasome system in vitro. Lys-PEG3-BA can be used for non-small cell lung cancer research.
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- CAS. Nr.: 3057939-67-7
- Formel: C38H57ClN9O7P
- Molecular Weight:818.34
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1975 | IC50 |
18.56 μM
Compound: Lys-PEG3-BA
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Inhibition of cell viability in human NCI-H1975 cells incubated for 48 to 72 hrs by CCK8 assay
Inhibition of cell viability in human NCI-H1975 cells incubated for 48 to 72 hrs by CCK8 assay
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[PMID: 39114932] |
In Vitro
Lys-PEG3-BA (0-20 μM) leads EML4-ALK decertation in H3122 (EML4-ALK) cells and attains a 91% reduction at 10 μM[2].
Lys-PEG3-BA (0-20 μM) specifically triggers the degradation of EGFR in H1975 (EGFR-L858R/T790M) cells, and attains a 52% reduction at 20 μM [2].
Lys-PEG3-BA (48-72 h) efficiently inhibits H3122 (EML4-ALK) and H1975 cell proliferation with an IC50s of 5.30 μM at 48 h and 18.56 μM at 72 h, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H1975 (EGFR-L858R/T790M) and H3122 (EML4-ALK)
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Concentration:0, 0.01, 0.1, 1, 10 and 20 μM
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Incubation Time:48 (for H3122) or 72 h (for H1975)
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Result:Specifically triggered the degradation of EGFR in H1975 (EGFR-L858R/T790M) cells, without affecting the wild-type EGFR protein level.
Resulted in apparent downregulation of the EML4 ALK protein in H3122 (EML4-ALK) cells at varying doses.
Chemical Information
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CAS. Nr. 3057939-67-7
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Molecular Weight 818.34
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Formel C38H57ClN9O7P
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SMILES
COC1=C(NC2=NC=C(Cl)C(NC3=C(C=CC=C3)P(C)(C)=O)=N2)C=CC(N4CCN(CC4)C(CCOCCOCCOCCNC([C@H](CCCCN)N)=O)=O)=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Chen X, et al. Mighty mini-PROTACs: an emerging class of degraders. Eur J Med Chem. 2026 Jan 5;301:118202. [Content Brief]
[2]. Zhang J, et al. Distinct Amino Acid-Based PROTACs Target Oncogenic Kinases for Degradation in Non-Small Cell Lung Cancer (NSCLC). J Med Chem. 2024 Aug 22;67(16):13666-13680. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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