2. PROTAC Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. PROTACs EGFR
  4. 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.

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Gly-PEG3-BA

Gly-PEG3-BA Chemical Structure

CAS No. : 3057939-66-6

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Gly-PEG3-BA Related Antibodies

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Description

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[1].

IC50 & Target[1]

EML4-ALK

 

In Vitro

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.

Gly-PEG3-BA Related Antibodies

Western Blot Analysis[1]

Cell Line: H1975 (harboring the EGFR L858R/ T790M double mutation), A549, H1299, PC9, H3122 (EML4-ALK) cells
Concentration: 0, 0.01, 0.1, 1, 10 and 20 μM
Incubation Time: 72 h
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.

Western Blot Analysis[1]

Cell Line: H3122 (EML-ALK), H1975 (EGER-L858R/T790M) cells
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
Incubation Time: 48 (for H3122 cell) or 72 h (for H1975 cell)
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.

Western Blot Analysis[1]

Cell Line: H3122 (EML-ALK), H1975 (EGER-L858R/T790M) cells
Concentration: 10 (for H3122) or 20 (for H1975) μM
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)
Result: led to a decrease in EML4-ALK or EGFR mutant protein levels at 15 min and 24 h.
Molecular Weight

747.22

Formula

C34H48ClN8O7P
CAS No.
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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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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Gly-PEG3-BA Related Classifications

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  • 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:

Gly-PEG3-BA3057939-66-6PROTACsEGFREpidermal growth factor receptorErbB-1HER1non-small lung cancer H3122 (EML4-ALK) cellsH1975 (L858R/T790M) cellsInhibitorinhibitorinhibit

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