UT-143
UT-143 is an orally active, selective irreversible covalent antagonist of androgen receptor (AR). UT-143 inhibits the proliferation of AR-positive prostate cancer cells, reduces the weight of androgen target tissues in rats, and suppresses the growth of AR-positive xenograft tumors. UT-143 can be used for the research of prostate cancer.
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- No. CAS: 2698320-33-9
- Fòrmula: C20H17F3N6O4
- Peso molecular:462.38
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Help & FAQs
Actividad biológica
UT-143 (10 µM; 16 h) significantly reduces genome-wide chromatin accessibility in 22RV1 prostate cancer cells, decreasing the number of accessible regions from 36141 to 10302[1].
UT-143 inhibits androgen receptor transcriptional activation with an IC50 value of 0.15 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 |
|---|---|---|---|
| Rat[1] | 20 mg/kg | p.o. | >12 h |
UT-143 (60 mg/kg; p.o.; daily; 18 days) potently inhibits the growth of AR-positive LNCaP-AR prostate cancer xenografts in intact male NSG mice, achieving over 95% tumor growth inhibition[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male)[1]
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Dosage:20 mg/kg
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Administration:p.o.; daily; 13 days
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Result:Reduced prostate weight to ~200 mg (vehicle control ~400 mg, P<0.01).
Reduced seminal vesicle weight to ~200 mg (vehicle control ~400 mg, P<0.01).
Had no effect on body weight, lean mass, fat mass, or the weights of the heart, kidney, spleen, and thymus.
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Animal Model:NSG (male)[1]
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Dosage:60 mg/kg
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Administration:p.o.; daily; 18 days
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Result:Achieved greater than 95% tumor growth inhibition, with tumor volume showing a net decrease from baseline over the treatment period.
Chemical Information
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No. CAS 2698320-33-9
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Peso molecular 462.38
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Fòrmula C20H17F3N6O4
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SMILES
N#CC(C=N1)=CN1C[C@@](OCC(C(OC)=O)=C)(C)C(NC2=CN=C(C#N)C(C(F)(F)F)=C2)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
UT-143 Related Classifications
HY-181427 Related Classifications
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