1. Vitamin D Related/Nuclear Receptor
  2. Androgen Receptor
  3. UT-105

UT-105 is an orally active androgen receptor (AR) degrader. UT-105 binds to the N-terminal domain of AR and promotes its degradation. UT-105 inhibits the growth of enzalutamide-resistant breast cancer xenografts and reduces tumor cell proliferation. UT-105 can be used in the research of estrogen receptor-positive breast cancer.

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

UT-105

UT-105 Chemical Structure

CAS No. : 2388536-21-6

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Description

UT-105 is an orally active androgen receptor (AR) degrader. UT-105 binds to the N-terminal domain of AR and promotes its degradation. UT-105 inhibits the growth of enzalutamide-resistant breast cancer xenografts and reduces tumor cell proliferation. UT-105 can be used in the research of estrogen receptor-positive breast cancer[1].

In Vivo

UT-105 (30 mg/kg; p.o.; daily; 30 days) significantly inhibits the growth of enzalutamide-resistant ER-positive breast cancer xenografts by reducing AR expression and tumor cell proliferation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NSG mice (6-8 week old female; orthotopic patient-derived xenograft model, enobosarm-resistant)[1]
Dosage: 30 mg/kg
Administration: p.o.; daily; 30 days
Result: Significantly inhibited growth of enobosarm-resistant WHIM23 tumors compared to vehicle- and enzalutamide-treated tumors.
Reduced percent change in tumor volume from day 0 significantly lower than vehicle controls.
Reduced AR protein levels in tumors.
Resulted in very low tumor cell proliferation measured by Ki67 immunohistochemistry.
Molecular Weight

364.28

Formula

C15H11F3N6O2

CAS No.
SMILES

N#CC(C=N1)=CN1C[C@](C)(O)C(NC2=CN=C(C#N)C(C(F)(F)F)=C2)=O

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UT-105
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HY-182722
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