2. PROTAC Protein Tyrosine Kinase/RTK Apoptosis
  3. PROTACs Anaplastic lymphoma kinase (ALK) Apoptosis
  4. ALK degrader 2

ALK degrader 2 is an orally active ALK degrader that degrades EML4-ALK levels (DC50 = 8 nM) and nucleophosmin (NPM)-ALK protein levels (DC50 = 102 nM). ALK degrader 2 mediates ALK degradation via the Hsp70 chaperone system and ubiquitin-proteasome pathway. ALK degrader 2 induces significant S-phase cell cycle arrest and apoptosis in H3122 cells. ALK degrader 2 shows anti-tumor activity in mice bearing H3122 xenografts. ALK degrader 2 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: ALK ligand (HY-W754809), Blue: Hyt (HY-W013021), Black: Linker (HY-Y1760), ALK ligand-linker conjugate (HY-175528)).

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ALK degrader 2

ALK degrader 2 Chemical Structure

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ALK degrader 2 Related Antibodies

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Description

ALK degrader 2 is an orally active ALK degrader that degrades EML4-ALK levels (DC50 = 8 nM) and nucleophosmin (NPM)-ALK protein levels (DC50 = 102 nM). ALK degrader 2 mediates ALK degradation via the Hsp70 chaperone system and ubiquitin-proteasome pathway. ALK degrader 2 induces significant S-phase cell cycle arrest and apoptosis in H3122 cells. ALK degrader 2 shows anti-tumor activity in mice bearing H3122 xenografts. ALK degrader 2 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: ALK ligand (HY-W754809), Blue: Hyt (HY-W013021), Black: Linker (HY-Y1760), ALK ligand-linker conjugate (HY-175528))[1].

In Vitro

ALK degrader 2 (Compound J26) (72 h) shows anti-proliferative effect on H3122 cells (IC50 = 25 nM)[1].
ALK degrader 2 (0.015-5 μM, 24 h) degrades EML4-ALK levels in H3122 cells (DC50 = 8 nM) and nucleophosmin (NPM)-ALK protein levels in SU-DHL-1 cells (DC50 = 102 nM)[1].
ALK degrader 2 (0.01-0.5 μM, 24 h) induces significant S-phase cell cycle arrest and apoptosis in H3122 cells[1].
ALK degrader 2 (0.5 μM, 24 h) mediates ALK degradation via the Hsp70 chaperone system and ubiquitin-proteasome pathway, without involving E3 ligases (CRBN, TTC3, ARK2N)[1].

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

ALK degrader 2 Related Antibodies

Apoptosis Analysis[1]

Cell Line: H3122 cells
Concentration: 0.01, 0.05, 0.5 μM
Incubation Time: 24 h
Result: Induced apoptosis in H3122 cells.

Cell Cycle Analysis[1]

Cell Line: H3122 cells
Concentration: 0.01, 0.05, 0.5 μM
Incubation Time: 24 h
Result: Induced significant S-phase cell cycle arrest in H3122 cells.
In Vivo

ALK degrader 2 (Compound J26) (10 mg/kg, i.v., single dose) significantly reduces EML4-ALK protein levels in tumor tissues at 24 h post-dose and sustains suppression up to 72 h in female BALB/c nude mice bearing H3122 xenografts[1].
ALK degrader 2 (20 mg/kg, p.o. or 5-10 mg/kg, i.v., once every other day for 21 days) shows anti-tumor activity in mice bearing H3122 xenografts[1].

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

Animal Model: H3122 cells (1 × 106 in appropriate volume) were subcutaneously implanted into the right flanks of 4-week-old female BALB/c nude mice to establish H3122 xenograft tumor models[1]
Dosage: 20 mg/kg (p.o.) or 5, 10 mg/kg (i.v.)
Administration: once every other day for 21 days
Result: Achieved tumor growth inhibition.
Showed no significant changes in body weight and no other signs of toxicity.
Significantly reduced EML4-ALK and phosphorylated ALK (p-ALK) protein levels in tumor tissues.
Induced significant tumor cell apoptosis.
Molecular Weight

644.85

Formula

C40H48N6O2
SMILES

O=C(CN1CCN(CC1)C2CCN(CC2)C3=C(C=C4C(C(C)(C5=C(C4=O)C(C=CC(C#N)=C6)=C6N5)C)=C3)CC)NCC7C8CC(C7)C=C8
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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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ALK degrader 2 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:

ALK degrader 2ALK degrader2ALK degrader-2PROTACsAnaplastic lymphoma kinase (ALK)ApoptosisAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246non-small cell lung cancer (NSCLC)ALKPROTACH3122 cellsInhibitorinhibitorinhibit

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