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

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Pro-PEG3-BA

Pro-PEG3-BA Chemical Structure

CAS No. : 3057939-64-4

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Pro-PEG3-BA Related Antibodies

Top Publications Citing Use of Products

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

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Description

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[1][2][3].

In Vitro

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.

Pro-PEG3-BA Related Antibodies

Western Blot Analysis [3]

Cell Line: H3122 cells (EML4-ALK), SK-N-BE(2) (express wild type ALK, and SH-SY5Y) and SH-SY5Y (harbors the ALK-F1174L)
Concentration: 0, 0.01, 0.1, 1, 10 and 20 μM
Incubation Time: 48 h
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.

Western Blot Analysis [3]

Cell Line: H3122 cells (EML4-ALK) and H1975 (EGFR L858R/T790M) cells
Concentration: 0.5 or 20 μM
Incubation Time: 6 h and 12 h
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).

Western Blot Analysis [3]

Cell Line: H3122 (10 μM) and H1975 (20 μM )
Concentration: H3122 (10 μM) and H1975 (20 μM)
Incubation Time: 0, 12, 24, 36, 48 and 72 h
Result: Induced the apparent reduction of EML4-ALK or EGFR mutant proteins, with effects observed around 45 min and 12 h.

Cell Cycle Analysis [3]

Cell Line: H3122 cells (EML4-ALK) and H1975 (EGFR L858R/T790M) cells
Concentration: 5 or 10 μM
Incubation Time: 48 (for H3122 cells) or 72 h (for H1975 cells)
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.
Parmacokinetics
Species Dose Route Tmax T1/2 Cmax AUC0-t F
Mice[3] 2 mg/kg i.v. 0.083 h 2.873 h 3.720 μg/mL 6.084 μg·h/mL /
Mice[3] 50 mg/kg i.p. 0.5 h 5.175 h 33.010 μg/mL 80.849 μg·h/mL 53.21 %
In Vivo

Pro-PEG3-BA (10 mg/kg, i.p., every other day for a total of 8 doses) decreases EML4-ALK expression with safety profile in a H3122 cells induced xenograft tumor mice model[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: H3122 cells induced-female nude mice[3]
Dosage: 10 mg/kg
Administration: i.p., every other day for a total of 8 doses
Result: Did not cause significant variations in the mice body weight.
Decreased EML4-ALK protein levels in tumors.
Molecular Weight

787.28

Formula

C37H52ClN8O7P
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]5CCCN5)=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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Pro-PEG3-BA Related Classifications

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  • Do most proteins show cross-species activity?

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Keywords:

Pro-PEG3-BA3057939-64-4PROTACsAnaplastic lymphoma kinase (ALK)EGFRApoptosisAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Epidermal growth factor receptorErbB-1HER1non-small cell lung cancerH3122EML4 ALKH1975NSCLCInhibitorinhibitorinhibit

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