Pro-PEG3-BA
Pro-PEG3-BA is an EML4-ALK/EGFR PROTAC degrader, degrading EML4 ALK and EGFR mutant (L858R/T790M) with DC50 values of 0.42 and 13.50 μM, respectively. Pro-PEG3-BA hinders proliferation and induces cell cycle arrest and apoptosis of NSCLC cells in vitro. Pro-PEG3-BA shows safety profile and decreases EML4-ALK protein via rewiring the ubiquitin- proteasome system in vivo. Pro-PEG3-BA can be used for non-small cell lung cancer research.
(Pink: EGFR and EML4-ALK ligand (HY-150908); Blue: Ligands for E3 Ligase ligand (HY-Y0252); Black: linker (HY-W040165)).
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- CAS No.: 3057939-64-4
- Formule: C37H52ClN8O7P
- Masse moléculaire:787.28
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1975 | IC50 |
8.8 μM
Compound: Pro-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] |
Pro-PEG3-BA (0-50 min) binds to purified ALK with a Kd of 387 nM in vitro [2]. Pro-PEG3-BA binds GID4 protein with Kd value of 6.05 μM in HEK293T cells[3].
Pro-PEG3-BA (0-20 μM, 48 h) specifically degradest EML4 ALK fusion in H3122 (EML4-ALK), with no effect on wild type or mutant ALK[3].
Pro-PEG3-BA (48-72 h) inhibits H3122 cells (48 h) prolifetion with an IC50 value of 0.16 μM, inhibits H1975 cells (EGFR-L858R/T790M) (72 h) prolifetion with an IC50 value of 8.80 μM[3].
Pro-PEG3-BA (48-72 h) inhibits cell growth with an IC50 value of 0.16 μM for H3122 (EML4-ALK) cells (48 h), and 8.8 μM for H1975 (EGFR-L858R/T790M) (72 h) cells, with little toxicity to normal cells (HEK293T cells)[3].
Pro-PEG3-BA (10 μM, 24 h) dramatically downregulates ALK protein abundance alongside CD2AP, MRPS23, RNF2, RAB18 and TRMT10C, demonstrating high selectivity in targeting ALK for degradation; concurrently, it upregulates POLR2F, WASHC2C, NCOR2, ZNF622, ALDH6A1, PRRC1, GPD1L, EXOC7, WACPAF1 in H1975 (EGFR L858R/T790M) cells[3].
Pro-PEG3-BA (10-20 μM, 0-24 h) induces the apparent reduction of EML4-ALK or EGFR mutant proteins in a time-dependent manner in H3122 (EML4-ALK) cells (10 μM) and H1975 (EGFR-L858R/T790M) cells (20 μM)[3].
Pro-PEG3-BA (0.5-20 μM, 6 or 12 h) reduces the levels of EML4-ALK and EGFR mutants in a proteasome-dependent manner in H3122 (EML4-ALK) and H1975 (EGFR-L858R/T790M) cells[3].
Pro-PEG3-BA (5-10 μM, 48-72 h) induces cell cycle arrest and apoptosis in H1975 (EGFR-L858R/T790M) cells and H3122 (EML4-ALK) cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H3122 cells (EML4-ALK), SK-N-BE(2) (express wild type ALK, and SH-SY5Y) and SH-SY5Y (harbors the ALK-F1174L)
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Concentration:0, 0.01, 0.1, 1, 10 and 20 μM
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Incubation Time:48 h
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Result:Led to a noticeable downregulation of the EML4-ALK protein in H3122 (EML4-ALK) cells.
Did not affect the protein levels of either wild-type or mutant ALK.
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Cell Line:H3122 cells (EML4-ALK) and H1975 (EGFR L858R/T790M) cells
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Concentration:0.5 or 20 μM
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Incubation Time:6 h and 12 h
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Result:Mediated the degradation of EML4-ALK or EGFR mutant, which was blocked by the proteasome inhibitor MG132 (HY-13259) (10 μM) instead of lysosome inhibitor Chloroquine (HY-17589A) (25 μM).
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Cell Line:H3122 (10 μM) and H1975 (20 μM )
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Concentration:H3122 (10 μM) and H1975 (20 μM)
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Incubation Time:0, 12, 24, 36, 48 and 72 h
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Result:Induced the apparent reduction of EML4-ALK or EGFR mutant proteins, with effects observed around 45 min and 12 h.
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Cell Line:H3122 cells (EML4-ALK) and H1975 (EGFR L858R/T790M) cells
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Concentration:5 or 10 μM
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Incubation Time:48 (for H3122 cells) or 72 h (for H1975 cells)
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Result:Induced an accumulation of cells in the G1 phase and concurrently causing a decrease in the number of cells in the S or G2 phase.
Significantly increased the proportion of both early and late apoptotic cells in a concentration-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:H3122 cells induced-female nude mice[3]
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Dosage:10 mg/kg
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Administration:i.p., every other day for a total of 8 doses
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Result:Did not cause significant variations in the mice body weight.
Decreased EML4-ALK protein levels in tumors.
Chemical Information
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CAS No. 3057939-64-4
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Masse moléculaire 787.28
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Formule C37H52ClN8O7P
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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]5CCCN5)=O)=O)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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. Linker-free PROTACs efficiently induce the degradation of oncoproteins. Nat Commun. 2025 May 23;16(1):4794. [Content Brief]
[3]. 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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pro-PEG3-BA Related Classifications
HY-180965 Related Classifications
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