Chemical Structure : T878A-mutant AR inhibitor S-94
CAS No.:
340259-91-8
T878A-mutant AR inhibitor S-94
货号: PC-26659Not For Human Use, Lab Use Only.
T878A-mutant AR inhibitor S-94 is a selective androgen receptor T878A-mutant androgen receptor (AR) antagonist, inhibits AR transcriptional activity (IC50=0.38 μM) and suppresses cell proliferation (IC50=10.32 μM) in LNCaP cells harboring the T878A-mutant AR.
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纯度 & COA & 质检文件 纯度:
>98% (HPLC)
生物&药学活性
T878A-mutant AR inhibitor S-94 is a selective androgen receptor T878A-mutant androgen receptor (AR) antagonist, inhibits AR transcriptional activity (IC50=0.38 μM) and suppresses cell proliferation (IC50=10.32 μM) in LNCaP cells harboring the T878A-mutant AR.
S-94 selectively targeted the T878A-mutant AR, exhibiting 50-fold greater potency against ART878A (IC50 = 0.49 μM) than against wild-type AR (IC50 = 27.18 μM).
S-94 antagonized several clinically relevant T878A-associated AR mutants, including ARF877L/T878A and ARH875Y/T878A, and displayed high selectivity over GR, MR, and PR.
S-94 (20 mg/kg, i.p.) inhibited tumor growth in an LNCaP xenograft model.
物理化学性质&存储条件
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分子量
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427.50
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分子式
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C26H25N3O3
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外观性状
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Solid
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CAS No.
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储存条件
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- 固体粉末
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-20°C 12 个月; 4°C 6 个月
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- 配置液
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-80°C 6 个月; -20°C 6 个月
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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phenyl (S)-(1-((3,5-dimethylphenyl)amino)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)carbamate
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参考文献
1. Zheng Y, et al. Eur J Med Chem. 2026 Apr 20;312:118862.
