Gly-PEG3-BA
Gly-PEG3-BA is an EML4-ALK PROTAC degrader. Gly-PEG3-BA effectively reduces EML4-ALK with a DC50 value of 0.50 μM in H3122 (EML4-ALK) cells. Gly-PEG3-BA effectively reduces EGFR mutant (L858R/T790M) levels with a DC50 of 20.15 μM in H1975 (EGER-L858R/T790M) cells. Gly-PEG3-BA exerts potent antiproliferation activity in H3122 (EML4-ALK) and H1975 (EGER-L858R/T790M) cells with IC50s value of 0.84 and 20.74 μM. Gly-PEG3-BA can be used for non-small lung cancer research.
(Pink: EGFR and EML4-ALK ligand (HY-150908); Blue: Ligands for E3 Ligase ligand (HY-Y0966); Black: linker (HY-W040165)).
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- No. CAS: 3057939-66-6
- Fòrmula: C34H48ClN8O7P
- Peso molecular:747.22
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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EML4-ALK |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1975 | IC50 |
20.72 μM
Compound: Gly-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] |
Gly-PEG3-BA (0-20 μM, 72 h) exhibits highly target-selective activity against EGFR in H1975 cells (harboring the EGFR L858R/ T790M double mutation) and induces dose-dependent targeted degradation of the EML4-ALK fusion protein in H3122 (EML-ALK) cells[1].
Gly-PEG3-BA (0-20 μM, 48 or 72 h) tune down EML4-ALK and EGFR mutant efficiently and confer potent antiproliferation activity in H3122 (EML-ALK) and H1975 (EGER-L858R/T790M) cells with IC50 values of 0.84 and 20.74 μM[1].
Gly-PEG3-BA (0-72 h, 48 or 72 h) effectively decreases EML4-ALK or EGFR mutant protein levels in a dose-dependent manner in H3122 and H1975 cells[1].
Gly-PEG3-BA induces the degradation of EML4-ALK and mutant EGFR, and this degradation process is mediated by ZYG11B and ZER1 in H3122 and H1975 cells (knocked down ZYG11B and ZER1 expression)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H1975 (harboring the EGFR L858R/ T790M double mutation), A549, H1299, PC9, H3122 (EML4-ALK) cells
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Concentration:0, 0.01, 0.1, 1, 10 and 20 μM
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Incubation Time:72 h
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Result:Triggered the degradation of EGFR without affecting the wild-type EGFR protein level in A549 and H1299 cells or the EGFR del19 mutant protein levels in PC9 cells.
Resulted an apparent downregulation of the EML4 ALK protein in H3122 cells at varying doses.
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Cell Line:H3122 (EML-ALK), H1975 (EGER-L858R/T790M) cells
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Concentration:0, 0.01, 0.1, 0.25, 0.5, 0.75, 1, 2.5, 5, 7.5, 10 μM, or 0, 10, 12.5, 15, 17.5 and 20 μM
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Incubation Time:48 (for H3122 cell) or 72 h (for H1975 cell)
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Result:Effectively reduced EML4-ALK in H3122 (EML-ALK) cells, with a DC50 value of 0.50 μM, and attained a 98% reduction at ∼10 μM.
Effectively reduced EGFR levels with DC50 of 20.15 μM and achieved a 43% at around 20 μM in H1975 (EGER-L858R/T790M) cells.
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Cell Line:H3122 (EML-ALK), H1975 (EGER-L858R/T790M) cells
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Concentration:10 (for H3122) or 20 (for H1975) μM
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Incubation Time:0, 0.25, 0.75, 1.5, 3, 6, 12 and 24 h (for H3122) or 0, 12, 24, 36, 48 and 72 h (for H1975)
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Result:led to a decrease in EML4-ALK or EGFR mutant protein levels at 15 min and 24 h.
Chemical Information
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No. CAS 3057939-66-6
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Peso molecular 747.22
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Fòrmula C34H48ClN8O7P
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SMILES
O=C(CN)NCCOCCOCCOCCC(N1CCN(CC1)C2=CC=C(C(OC)=C2)NC3=NC=C(C(NC4=C(P(C)(C)=O)C=CC=C4)=N3)Cl)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. 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]
[2]. Chen X, et al. Mighty mini-PROTACs: an emerging class of degraders. Eur J Med Chem. 2026 Jan 5;301:118202. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Gly-PEG3-BA Related Classifications
HY-180966 Related Classifications
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