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Chemical Structure : NCT-58
CAS No.: 2411429-33-7
Catalog No.: 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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|---|---|---|---|
| 5 mg | $348 | In stock | |
| 10 mg | $558 | In stock | |
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| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 466.58 | |
| Formula | C27H34N2O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
5-methoxy-N-(3-methoxy-4-(2-(piperidin-2-yl)ethoxy)phenyl)-2,2-dimethyl-2H-chromene-6-carboxamide |
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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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