2. PROTAC Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. PROTACs Anaplastic lymphoma kinase (ALK) EGFR
  4. 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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Lys-PEG3-BA

Lys-PEG3-BA Chemical Structure

CAS No. : 3057939-67-7

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Lys-PEG3-BA Related Antibodies

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

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Description

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[1][2].

Cellular Effect
Cell Line Type Value Description References
NCI-H1975 IC50
18.56 μM
Compound: Lys-PEG3-BA
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
[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.

Lys-PEG3-BA Related Antibodies

Western Blot Analysis[2]

Cell Line: H1975 (EGFR-L858R/T790M) and H3122 (EML4-ALK)
Concentration: 0, 0.01, 0.1, 1, 10 and 20 μM
Incubation Time: 48 (for H3122) or 72 h (for H1975)
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.
Molecular Weight

818.34

Formula

C38H57ClN9O7P
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Lys-PEG3-BA Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lys-PEG3-BA3057939-67-7PROTACsAnaplastic lymphoma kinase (ALK)EGFRAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Epidermal growth factor receptorErbB-1HER1ubiquitin- proteasome systemnon-small cell lung cancerInhibitorinhibitorinhibit

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