2. Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  3. Androgen Receptor HSP
  4. 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.

Androgen receptor degrader-6

Androgen receptor degrader-6 Chemical Structure

CAS No. : 1372688-55-5

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Androgen receptor degrader-6 Related Antibodies

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Description

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[1].

In Vitro

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.

Androgen receptor degrader-6 Related Antibodies

Cell Viability Assay[1]

Cell Line: AR-overexpressing GBM cell lines T98G, U87; patient-derived GBM cell line DI318
Concentration: /
Incubation Time: 48 h
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.
Parmacokinetics
Species Dose Route Cmax AUC0-24 AUC0-∞ T1/2
Mice[1] 20 (Plasma) mg/kg i.p. 18.15 μg/mL 9.27 μg·h/mL 9.68 μg·h/mL 3.11 h
Mice[1] 20 (Brain) mg/kg i.p. 6.68 μg/g 4.90 μg·h/g 5.01 μg·h/g /
In Vivo

Androgen receptor degrader-6 (20 mg/kg; i.p.; three times per week for 14 days) significantly inhibits the growth of subcutaneous glioblastoma xenografts in nude mice, reduces AR protein levels in tumors, and causes no observed systemic toxicity[1].
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.

Animal Model: NCRNU nude mice (male, 5-6 weeks old, n=4 per group, subcutaneous glioblastoma xenograft model)[1]
Dosage: 20 mg/kg
Administration: i.p.; three times per week; 14 days
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.
Molecular Weight

396.41

Formula

C17H20N2O7S
CAS No.
SMILES

CN(S(C)(=O)=O)C1=CC=C([N+]([O-])=O)C=C1OCC2=CC(OC)=CC=C2OC
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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Androgen receptor degrader-6 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:

Androgen receptor degrader-61372688-55-5Androgen receptor degrader6Androgen receptor degrader 6Androgen ReceptorHSPHeat shock proteinsHSP27DI318T98Gandrogen receptorU87AR-V7nude miceSer78 phosphorylationblood-brain barrierglioblastomaInhibitorinhibitorinhibit

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