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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Androgen Receptor (AR)-UT-105
UT-105

Chemical Structure : UT-105

CAS No.: 2388536-21-6

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UT-105 (UT105)

货号: PC-21404Not For Human Use, Lab Use Only.

UT-105 is a small-molecule, irreversible, selective androgen receptor (AR) degrader (SARD) and irreversible inhibitor, binds to AR N-terminal domain (NTD) and inhibits both the AR and AR splice variants (AR-SVs).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

UT-105 is a small-molecule, irreversible, selective androgen receptor (AR) degrader (SARD) and irreversible inhibitor, binds to AR N-terminal domain (NTD) and inhibits both the AR and AR splice variants (AR-SVs).
UT-105 selectively inhibits wild-type and enzalutamide-resistant mutant AR transactivation with IC50 of 59.4 nM and 36.5 nM, respectively.
UT-105 is selective to AR and does not inhibit the transactivation of glucocorticoid (GR) or mineralocorticoid (MR) receptors in a panel of kinases (468) and 168 GPCRs.
UT-105 binds to AR NTD, but not ligand-binding domain (LBD).
UT-105 effectively degrades AR, irreversibly inhibits AR, inhibits AR-target genes, and significantly inhibits proliferation and colony formation in cells expressing AR and AR-V7.
UT-105 (60 mg/kg/day), but not enzalutamide and bicalutamide, inhibits TNBC tumor growth in orthotopic MDA-MB-453 TNBC model with a tumor growth inhibition (TGI) of >90%.
UT-105 inhibits STAT1 phosphorylation, effectively reduces IRF1, IRF7, and IRF9 expression in tumors, also inhibits the phosphorylation of STAT1, STAT3, and AKT in MDA-MB-453 tumors.

物理化学性质&存储条件

分子量 364.29
分子式 C15H11F3N6O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(S)-3-(4-cyano-1H-pyrazol-1-yl)-N-(6-cyano-5-(trifluoromethyl)pyridin-3-yl)-2-hydroxy-2-methylpropanamide

参考文献

1. Asemota S, et al. Cell Rep. 2023 Nov 17;42(12):113461.

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