Androgen receptor degrader-6
Androgen receptor degrader-6 is a blood-brain barrier-permeable AR degrader. Androgen receptor degrader-6 inhibits the chaperone activity of HSP27 and disrupts the HSP27-AR complex. Androgen receptor degrader-6 promotes the degradation of wild-type and mutant AR, reduces AR protein levels, and inhibits the growth of glioblastoma cells. Androgen receptor degrader-6 can be used in glioblastoma research.
For research use only. We do not sell to patients.
- CAS No.: 1372688-55-5
- Formula: C17H20N2O7S
- Molecular Weight:396.41
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Androgen receptor degrader-6 (compound A) (48 h) inhibits the growth of T98G, U87 and DI318 glioblastoma (GBM) cells[1].
Androgen receptor degrader-6 (0.5-2 μM) dose-dependently reduces the protein level of wild-type AR in U87, T98G and DI318 glioblastoma (GBM) cells, and decreases the protein level of mutant AR-V7 in T98G GBM cells[1].
Androgen receptor degrader-6 (0.5-1 μM; 30 min heat shock at 42 °C) inhibits phosphorylation of HSP27 at Ser78 in T98G and U87 glioblastoma (GBM) cells, but has no effect on phosphorylation at Ser82[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AR-overexpressing GBM cell lines T98G, U87; patient-derived GBM cell line DI318
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Concentration:/
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Incubation Time:48 h
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Result:Inhibited T98G cell growth with an IC50 of 240 nM.
Inhibited U87 cell growth with an IC50 of 850 nM.
Inhibited DI318 cell growth with an IC50 of 2.88 μM.
Androgen receptor degrader-6 (200 mg/kg; i.p.; once daily; for 10 consecutive days) shows no toxicity in C57BL/6 mice, with stable body weight, normal hematological parameters and no abnormal histomorphology of organs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NCRNU nude mice (male, 5-6 weeks old, n=4 per group, subcutaneous glioblastoma xenograft model)[1]
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Dosage:20 mg/kg
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Administration:i.p.; three times per week; 14 days
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Result:Significantly reduced xenograft tumor volume compared to vehicle control.
Reduced tumor weight compared to vehicle control.
Significantly reduced AR protein expression in tumor tissues compared to vehicle control.
Showed no significant change in mouse body weight relative to vehicle control.
Chemical Information
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CAS No. 1372688-55-5
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Molecular Weight 396.41
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Formula C17H20N2O7S
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SMILES
CN(S(C)(=O)=O)C1=CC=C([N+]([O-])=O)C=C1OCC2=CC(OC)=CC=C2OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Androgen receptor degrader-6 Related Classifications
HY-182809 Related Classifications
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