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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Estrogen Receptor/ERR-T6I-29
T6I-29

Chemical Structure : T6I-29

CAS No.: 2824308-33-8

T6I-29 (Selective estrogen receptor modulator)

货号: PC-22503Not For Human Use, Lab Use Only.

T6I-29 is a novel isoquinoline-based selective estrogen receptor modulator (SERM), interacts with Y537S ERα ligand binding domain (LBD), exhibits anti-proliferative activities, downregulates target genes, and elicits anti-tumoral activities.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

T6I-29 is a novel isoquinoline-based selective estrogen receptor modulator (SERM), interacts with Y537S ERα ligand binding domain (LBD), exhibits anti-proliferative activities, downregulates target genes, and elicits anti-tumoral activities.
T6I-29 demonstrates significant anti-proliferative activities in Y537S ERα breast cancer cells.
T6I-29 inhibits WT and Y537S ERα-Coactivator binding.
T6I-29 uniquely downregulates DKK1 in Y537S ESR1 breast cancer cells.
The active enantiomer of T6I-29, T6I-29-1A (25 mg/kg) inhibits tumor growth in ESR1 MCF7 Y537S xenograft model.

物理化学性质&存储条件

分子量 514.64
分子式 C32H35FN2O3
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

(1'-(4-((1-(3-fluoropropyl)pyrrolidin-3-yl)methoxy)phenyl)-6'-hydroxy-1',4'-dihydro-2'H-spiro[cyclopropane-1,3'-isoquinolin]-2'-yl)(phenyl)methanone

参考文献

1. Young KS, et al. bioRxiv [Preprint]. 2024 Jun 2:2024.05.28.596307.

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