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Referencia número: HY-182722

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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.

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No. CAS: 2388536-21-6
Fòrmula: C₁₅H₁₁F₃N₆O₂
Peso molecular:364.28

Almacenamiento:

Please store the product under the recommended conditions in the Certificate of Analysis.

UT-105 Chemical Structure

No. CAS: 2388536-21-6

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Actividad biológica
- Descripciòn
- In Vivo
Chemical Information
Pureza y Documentación
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Actividad biológica

Descripciòn

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.

Chemical Information

No. CAS 2388536-21-6
Peso molecular 364.28
Fòrmula C₁₅H₁₁F₃N₆O₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Asemota S, et al. A molecular switch from tumor suppressor to oncogene in ER+ve breast cancer: Role of androgen receptor, JAK-STAT, and lineage plasticity. Proc Natl Acad Sci U S A. 2024;121(40):e2406837121. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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