UT-105
UT-105 is an orally active, selective androgen receptor (AR) degrader. UT-105 binds to the N-terminal domain of AR, inhibits the transactivation of AR, blocks the recruitment of AR to androgen response elements, and induces AR degradation. UT-105 inhibits the JAK-STAT signaling pathway, including reducing the expression of interferon-stimulated genes, inhibiting the phosphorylation of STAT1 and STAT3, and blocking the recruitment of STAT1 to response elements. UT-105 exhibits anticancer activity against AR-positive triple-negative breast cancer (TNBC). UT-105 can be used in the research of selective androgen receptor modulator-resistant ER-positive breast cancer and triple-negative breast cancer.
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- CAS No.: 2388536-21-6
- Formule: C15H11F3N6O2
- Masse moléculaire:364.28
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
IC50 & Target
[2]|
STAT1 |
STAT3 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COS-7 | IC50 |
59.4 nM
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Inhibition of wild-type AR transactivation in COS7 cells in the presence of 0.1 nM synthetic androgen agonist R1881, measured via luciferase assay after 24 h treatment.
Inhibition of wild-type AR transactivation in COS7 cells in the presence of 0.1 nM synthetic androgen agonist R1881, measured via luciferase assay after 24 h treatment.
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37979170 |
| COS-7 | IC50 |
36.5 nM
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Inhibition of enzalutamide-resistant AR F876L transactivation in COS7 cells in the presence of 0.1 nM synthetic androgen agonist R1881, measured via luciferase assay after 24 h treatment.
Inhibition of enzalutamide-resistant AR F876L transactivation in COS7 cells in the presence of 0.1 nM synthetic androgen agonist R1881, measured via luciferase assay after 24 h treatment.
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37979170 |
In Vitro
UT-105 (24 h) potently inhibits wild-type and Enzalutamide (HY-70002)-resistant mutant AR transactivation in COS7 cells, with IC50 values of 59.4 nM and 36.5 nM, respectively, and shows no cross-reactivity with GR or MR[2].
UT-105 (1-10 μM; 24 h) degrades AR protein in LNCaP prostate cancer cells when treated in the presence of 0.1 nM R1881[2].
UT-105 (10 μM; overnight at 4°C for binding assay; 100 μM; 4 h at room temperature for stabilization assay) binds to the AR NTD, inducing a conformational change, and stabilizes purified AR AF-1 and AR-V7 proteins in cell-free biochemical assays[2].
UT-105 (3 μM; 20 h) reverses androgen-responsive gene expression and significantly downregulates the androgen response pathway in MDA-MB-453 LAR TNBC cells when treated in the presence of 0.1 nM R1881[2].
UT-105 (10 μM; 2 weeks) inhibits colony formation in AR-V7-expressing MDA-MB-453-V7, MDA-MB-231-V7, and MFM223-V7 TNBC cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LNCaP prostate cancer cells
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Concentration:1-10 μM (in presence of 0.1 nM R1881)
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Incubation Time:24 h
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Result:Downregulated AR protein expression in a concentration-dependent manner relative to vehicle control.
In Vivo
UT-105 (60 mg/kg; p.o.; once daily; for 28 consecutive days) potently inhibits the growth of MDA-MB-453 LAR TNBC xenografts, with a tumor growth inhibition rate of >90%[2].
UT-105 (60 mg/kg; p.o.; once daily; for 28 consecutive days) potently inhibits the growth of the UT-1355 LAR-AR-SV triple-negative breast cancer PDX model, with a tumor growth inhibition rate >90% and reduced tumor weight[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG (female)[2]
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Dosage:60 mg/kg
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Administration:p.o.; daily; 28 days
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Result:Achieved >90% tumor growth inhibition (TGI).
Showed no effect on body weight of tumor-bearing mice.\nAchieved >90% tumor growth inhibition (TGI).
Showed no effect on body weight of tumor-bearing mice.
Significantly reduced tumor weights compared with vehicle and enzalutamide groups.
Chemical Information
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CAS No. 2388536-21-6
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Masse moléculaire 364.28
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Formule C15H11F3N6O2
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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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
UT-105 Related Classifications
HY-182722 Related Classifications
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Keywords
- UT-105
- 2388536-21-6
- UT105
- UT 105
- Androgen Receptor
- JAK
- STAT
- triple-negative breast cancer
- androgen receptor
- human wild-type AR
- human AR F876L mutant
- selective androgen receptor modulator-resistant breast cancer
- JAK-STAT signaling pathway
- AR-V7
- LNCaP prostate cancer cells
- COS7 cells
- MDA-MB-453 LAR TNBC cells
- Inhibitor
- inhibitor
- inhibit