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製品番号: 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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CAS 番号: 2388536-21-6
分子式: C₁₅H₁₁F₃N₆O₂
分子量:364.28

保管条件:

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

UT-105 構造式

CAS 番号: 2388536-21-6

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性

製品説明

体内実験

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.

化学情報

CAS 番号 2388536-21-6
分子量 364.28
分子式 C₁₅H₁₁F₃N₆O₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[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.

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100 mg

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