2. Vitamin D Related/Nuclear Receptor
  3. Androgen Receptor
  4. 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.

For research use only. We do not sell to patients.

UT-143

UT-143 Chemical Structure

CAS No. : 2698320-33-9

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UT-143 Related Antibodies

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Description

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[1].

In Vitro

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.

UT-143 Related Antibodies
Parmacokinetics
Species Dose Route T1/2
Rat[1] 20 mg/kg p.o. >12 h
In Vivo

UT-143 (20 mg/kg; p.o.; daily; 13 days) potently inhibits androgen-dependent prostate and seminal vesicle growth in intact male Sprague-Dawley rats without altering body weight or non-target organ weights[1].
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.

Animal Model: Sprague-Dawley (male)[1]
Dosage: 20 mg/kg
Administration: p.o.; daily; 13 days
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.
Animal Model: NSG (male)[1]
Dosage: 60 mg/kg
Administration: p.o.; daily; 18 days
Result: Achieved greater than 95% tumor growth inhibition, with tumor volume showing a net decrease from baseline over the treatment period.
Molecular Weight

462.38

Formula

C20H17F3N6O4
CAS No.
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
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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UT-143 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:

UT-1432698320-33-9UT143UT 143Androgen ReceptorC327androgen receptor22RV1 prostate cancer cellsSprague-Dawley ratsprostate cancer cellsC406LNCaP-AR prostate cancer xenograftsAR-V7NSG miceSRC-3Inhibitorinhibitorinhibit

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