2. PROTAC Apoptosis Protein Tyrosine Kinase/RTK
  3. PROTACs Apoptosis Anaplastic lymphoma kinase (ALK)
  4. PROTAC EML4-ALK Degrader-1

PROTAC EML4-ALK Degrader-2 (Pro-BA) is a selective and orally active linker-free EML4-ALK PROTAC degrader with the DC50 of 74 nM in H1322 cells (T1/2 = 8 h). PROTAC EML4-ALK Degrader-2 relies on GID4 and proteasome pathways to promote ubiquitination of target proteins, leading to cell apoptosis. PROTAC EML4-ALK Degrader-2 can be used for research on cancer. (Pink: EML4-ALK Ligand (HY-40114); Blue: GID4 Ligand (HY-150908))

For research use only. We do not sell to patients.

PROTAC EML4-ALK Degrader-1 Chemical Structure

PROTAC EML4-ALK Degrader-1 Chemical Structure

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PROTAC EML4-ALK Degrader-1 Related Antibodies

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Description

PROTAC EML4-ALK Degrader-2 (Pro-BA) is a selective and orally active linker-free EML4-ALK PROTAC degrader with the DC50 of 74 nM in H1322 cells (T1/2 = 8 h). PROTAC EML4-ALK Degrader-2 relies on GID4 and proteasome pathways to promote ubiquitination of target proteins, leading to cell apoptosis. PROTAC EML4-ALK Degrader-2 can be used for research on cancer. (Pink: EML4-ALK Ligand (HY-40114); Blue: GID4 Ligand (HY-150908)) [1]

In Vitro

PROTAC EML4-ALK Degrader-2 (Compound Pro-BA) (0-1 μM; 0-24 h) can significantly and selectively degrade the levels of EML4-ALK in H3122 (DC50 = 74 nM), BaF3-EML4-ALK (DC50 = 125 nM) and neuroblastoma SK-N-BE(2) cells (DC50 = 2.1 μM)[1].
PROTAC EML4-ALK Degrader-2 (500 nM; 24 h) increases the proportion of G1 phase cells and significantly increases cell apoptosis in H3122 cells[1].
PROTAC EML4-ALK Degrader-2 (500 nM; 24 h) induces the degradation of EML4-ALK through the ubiquitin-proteasome system in HEK293T cells.[1].

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

PROTAC EML4-ALK Degrader-1 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: H3122 cells
Concentration: 500 nM
Incubation Time: 24 h
Result: Increased the proportion of G1 phase cells.

Cell Viability Assay[1]

Cell Line: H3122 cells
Concentration: 0-1 μM
Incubation Time: 48 h
Result: Significantly inhibited the growth of H3122 cells (IC50 = 34 nM).

Apoptosis Analysis[1]

Cell Line: H3122 cells
Concentration: 500 nM
Incubation Time: 24 h
Result: Significantly increased the proportion of early and late apoptosis.
In Vivo

PROTAC EML4-ALK Degrader-2 (Compound Pro-BA) (10 mg/kg; i.p.; every other day; a total of 8 doses) significantly reduces the level of EML4-ALK and inhibits tumor growth in the female nude mice with H3122 xenograft tumors[1].
PROTAC EML4-ALK Degrader-2 (25 mg/kg; p.o.; every two days; a total of 8 doses) reduces the level of EML4-ALK and inhibits tumor growth, and exhibits low toxicity in the female nude mice with H3122 xenograft tumors[1].

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

Animal Model: 1×107 H3122 cells injected female nude mice (4 weeks)[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.); every other day for a total of 8 doses
Result: Significantly reduced the level of EML4-ALK protein in tumors.
Had good tolerance and no significant change in weight.
Significantly inhibits the volume of tumors.
Animal Model: 1×107 H3122 cells injected female nude mice (4 weeks)[1]
Dosage: 25 mg/kg
Administration: Oral administration (p.o.); every two days for a total of 8 doses
Result: Significantly reduced the level of EML4-ALK protein in tumors.
Significantly inhibits the volume of tumors.
Did not change the structure in the main organs.
Molecular Weight

584.05

Formula

C28H35ClN7O3P
SMILES

COC1=C(C=CC(N2CCN(CC2)C([C@H]3CCCN3)=O)=C1)NC4=NC=C(C(NC5=CC=CC=C5P(C)(C)=O)=N4)Cl
Shipping

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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PROTAC EML4-ALK Degrader-1 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:

PROTAC EML4-ALK Degrader-1Pro-BAPROTACsApoptosisAnaplastic lymphoma kinase (ALK)Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246EML4-ALKPROTACUbiquitinationCancerapoptosisH1322Inhibitorinhibitorinhibit

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