NCT-58

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

NCT-58 是一种有效的 C 端 HSP90 抑制剂。 NCT-58 不会诱发热休克反应 (HSR)。

NCT-58 is a potent C-terminal HSP90 inhibitor. NCT-58 does not induce the heat shock response (HSR). NCT-58 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.(In Vitro):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 (0.1-20?μM;?72 hours) dose-dependently reduces cell viability 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 .(In Vivo):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. NCT-58 (30?mg/kg; i.p.; every other day for 47 days) suppresses Trastuzumab-resistant tumor growth.

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. Cell Viability Assay Cell Line:BT474 and SKBR3 cells Concentration:0, 0.1, 0.5, 1, 5, 10, 15, 20?μM Incubation Time:72 hours Result:Significantly reduced cell growth.Apoptosis Analysis Cell Line:BT474 and SKBR3 cells Concentration:0, 2, 10 μM Incubation Time:72 hours Result:Increased the number of early and late apoptotic cells.Western Blot Analysis Cell Line:Trastuzumab-resistant JIMT-1 and MDA-MB-453 cells Concentration:0, 2, 10 μM Incubation Time:72 hours Result: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.

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.

NCT58

Cytoskeleton/Cell Adhesion Molecules

HSP

HSP

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2411429-33-7

466.57

C27H34N2O5

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (107.17 mM)

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(-20℃)

With Ice Pack

≥ 2 years