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)).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C40H48N6O2
- Masse moléculaire:644.85
-
Stockage:
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]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
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.
-
Cell Line:H3122 cells
-
Concentration:0.01, 0.05, 0.5 μM
-
Incubation Time:24 h
-
Result:Induced apoptosis in H3122 cells.
-
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.
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.
Chemical Information
-
Masse moléculaire 644.85
-
Formule 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
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ALK degrader 2 Related Classifications
HY-175527 Related Classifications
Powered by Bioz