HEMTAC AR degrader-1
HEMTAC AR degrader-1 is an androgen receptor (AR) HEMTAC degrader that recruits HSP70, with a Kd value of 825 nM for HSP72. HEMTAC AR degrader-1 induces AR degradation, and inhibits the proliferation and migration of cancer cells. HEMTAC AR degrader-1 can be used in the research of prostate cancer.
(Pink: Androgen Receptor Target protein ligand; Blue: HSP70 E3 ligase ligand; Black: linker).
For research use only. We do not sell to patients.
- Formula: C44H44ClF3N10O7
- Molecular Weight:917.33
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Storage:
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
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
HEMTAC AR degrader-1 (Compound 39) (0.1-10 μM; 1-24 h) induces potent, time-dependent, and proteasome-mediated AR degradation in LNCaP prostate cancer cells, reducing AR levels by 89% after treatment at 5 μM for 24 h[1].
HEMTAC AR degrader-1 (72 h) potently inhibits the proliferation of LNCaP prostate cancer cells with an IC50 of 2.20 μM, whereas it exhibits only limited activity in AR-deficient PC-3 cells and non-tumorigenic HFF-1 fibroblasts[1].
HEMTAC AR degrader-1 (1-5 μM; 7 days) impairs the long-term reproductive viability of LNCaP prostate cancer cells in a dose-dependent manner[1].
HEMTAC AR degrader-1 (1-5 μM; 48 h) inhibits the migratory capacity of LNCaP prostate cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LNCaP androgen-dependent prostate cancer cells
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Concentration:0.1, 0.5, 1, 5, 10 μM (24 h); 5 μM (time-course)
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Incubation Time:24 h (0.1, 0.5, 1, 5, 10 μM); 1 h, 3 h, 6 h, 12 h, 24 h (5 μM)
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Result:Induced an 89% reduction in AR protein levels at 5 μM for 24 h.
Induced an 88% reduction in AR protein levels at 10 μM for 24 h.
Showed significant AR degradation within 12 h in time-dependent analysis with 5 μM.
Abolished AR degradation when cells were pretreated with proteasome inhibitor MG132, confirming proteasome-mediated activity.
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Cell Line:LNCaP androgen-dependent prostate cancer cells
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Concentration:1 and 5 μM
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Incubation Time:7 days
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Result:Dose-dependently inhibited colony formation, with a significant reduction in colony number at 5 μM compared to vehicle control and individual reference ligands.
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Cell Line:LNCaP androgen-dependent prostate cancer cells
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Concentration:1 and 5 μM
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Incubation Time:48 h
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Result:Inhibited the migratory capacity of LNCaP prostate cancer cells at micromolar. concentrations
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Four-week-old male BALB/c nude mice[1]
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Dosage:10 and 20 mg/kg
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Administration:i.p.; once daily for 14 consecutive days
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Result:Dosage-dependly inhibited tumor growth, with no obvious toxicity.
Chemical Information
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Molecular Weight 917.33
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Formula C44H44ClF3N10O7
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SMILES
CC1=NN(C2=CC=C(C#N)C(C(F)(F)F)=C2)C(C)=C1CC3=CC=C(C(NCCCCNC(COC4=NC=NC5=C4N=C(NCC6=CC=C(Cl)C=C6)N5[C@H]7[C@H](O)[C@H](O)[C@@H](CO)O7)=O)=O)C=C3
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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)
HEMTAC AR degrader-1 Related Classifications
HY-187229 Related Classifications
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