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编 号:F741557
分子式:C27H34N2O5
分子量:466.57
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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生物活性:
NCT-58 is a potent inhibitor of C-terminal HSP90. NCT-58 does not induce the heat shock response (HSR) due to its targeting of the C-terminal region and elicits anti-tumor activity via the simultaneous downregulation of HER family members as well as inhibition of Akt phosphorylation. NCT-58 kills Trastuzumab-resistant breast cancer stem-like cells. NCT-58 induces apoptosis in HER2-positive breast cancer cells.

体内研究:
NCT-58 (30?mg/kg; i.p.; every other day for 47 days) suppresses Trastuzumab-resistant tumor growth.NCT-58 (30?mg/kg; i.p.; every other day for 47 days) causes a significant impediment of tumor growth and a marked decrease in tumor weight.Animal Model:Trastuzumab-resistant xenograft model (female nude mice; 6 weeks; BALB/c)
Dosage:30?mg/kg
Administration:i.p.; every other day for 47 days
Result:Significantly reduced tumor growth.

体外研究:
NCT-58 treatment (0.1-20?μM;?72 hours) dose-dependently reduces cell viability in HER2-positive BT474 and SKBR3 cells. NCT-58 treatment (0.1-10?μM;?72 hours) increases the number of early and late apoptotic cells in HER2-positive BT474 and SKBR3 cells.NCT-58 treatment (2-10?μM;?72 hours) effectively reduced the levels of truncated p95HER2 and its phosphorylated form, as well as downregulation of Akt and phospho-Akt (Ser473) protein contents in JIMT-1 and MDA-MB-453 cells.
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