ALK degrader 2
ALK degrader 2 is an orally active ALK HyT 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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- 화학식: C40H48N6O2
- 분자량:644.85
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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.
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Cell Line:H3122 cells
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Concentration:0.01, 0.05, 0.5 μM
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Incubation Time:24 h
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Result:Induced apoptosis in H3122 cells.
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Cell Line:H3122 cells
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Concentration:0.01, 0.05, 0.5 μM
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Incubation Time:24 h
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Result:Induced significant S-phase cell cycle arrest in H3122 cells.
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.
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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]
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Dosage:20 mg/kg (p.o.) or 5, 10 mg/kg (i.v.)
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Administration:once every other day for 21 days
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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.
Chemical Information
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분자량 644.85
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화학식 C40H48N6O2
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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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ALK degrader 2 Related Classifications
HY-175527 Related Classifications
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