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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Heat Shock Protein (HSP)-NCT-58
NCT-58

Chemical Structure : NCT-58

CAS No.: 2411429-33-7

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NCT-58 (C-terminal HSP90 inhibitor)

货号: PC-22213Not For Human Use, Lab Use Only.

NCT-58 is a specfiic small molecule C-terminal HSP90 inhibitor, kills trastuzumab-resistant HER2-positive breast cancer stem-like cells, targets the C-terminal HSP90 without inducing heat shock response (HSR).

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10 mg ￥5580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

NCT-58 is a specfiic small molecule C-terminal HSP90 inhibitor, kills trastuzumab-resistant HER2-positive breast cancer stem-like cells, targets the C-terminal HSP90 without inducing heat shock response (HSR).
NCT-58 exhibits significant inhibition of cell proliferation in HER2-positive breast cancer cells, with an IC50 = 8.53 and 4.45 μM in BT474 and JIMT1, respectively, with minimal cytotoxicity in normal HEK293 cells.
NCT-58 targets the C-terminal domain of HSP90 and downregulates HER2, HER3, and EGFR expression.
NCT-58 induces apoptosis and inhibits tyrosine kinase activity of HER2 in trastuzumab-resistant cells.
NCT-58 eradicates HER2-positive BCSCs without triggering the HSR.
NCT-58 (30 mg/kg) inhibits tumor growth in trastuzumab-resistant JIMT-1 xenografts, suppresses BCSC-like properties and downregulates the expression of HSF-1, HSP70, and HSP90 in vivo.

物理化学性质&存储条件

分子量 466.58
分子式 C27H34N2O5
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

5-methoxy-N-(3-methoxy-4-(2-(piperidin-2-yl)ethoxy)phenyl)-2,2-dimethyl-2H-chromene-6-carboxamide

参考文献

1. Soeun Park, et al. Cell Death Discov. 2021 Nov 13;7(1):354.

2. Nguyen CT, et al. Bioorg Med Chem Lett. 2020;30:127374.

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