2388536-21-6
Chemical Structure
UT-105
- CAS No.: 2388536-21-6
- Formula:C15H11F3N6O2
- Molecular Weight:364.28
InChIKey: KKMPHQUSORVAPU-AWEZNQCLSA-N
SMILES: N#CC(C=N1)=CN1C[C@](C)(O)C(NC2=CN=C(C#N)C(C(F)(F)F)=C2)=O
Biological Activity: 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[1][2].
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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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References
- [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. Proceedings of the National Academy of Sciences of the United States of America. 2024 Oct;121(40):e2406837121. [Content Brief]
- [2]. Asemota S, et al. Identification of a targetable JAK-STAT enriched androgen receptor and androgen receptor splice variant positive triple-negative breast cancer subtype. Cell reports. 2023 Dec 26;42(12):113461.
