NCT-58

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

NCT-58 

NCT-58是 HSP90 C末端的有效抑制剂。NCT-58 不诱导热休克反应 (HSR)，因为它靶向 C 末端区域，并通过同时下调 HER 家族成员以及抑制 Akt 磷酸化来引发抗肿瘤活性。NCT-58 可杀死曲妥珠单抗耐药 (Trastuzumab-resistant) 的乳腺癌干细胞样细胞。NCT-58 诱导 HER2 阳性乳腺癌细胞凋亡。在抗曲妥珠单抗异种移植模型中，NCT-58 可抑制生长和血管生成。

NCT-58

NCT-58 Chemical Structure

CAS No. : 2411429-33-7

规格 价格 是否有货
5 mg ￥4600 询问价格 & 货期
10 mg ￥7500 询问价格 & 货期
25 mg ￥14500 询问价格 & 货期

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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[1].

IC50 & Target[1]

HSP90

 

Apoptosis

 

体外研究
(In Vitro)

NCT-58 treatment (0.1-20 μM; 72 hours) dose-dependently reduces cell viability in HER2-positive BT474 and SKBR3 cells[1].
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[1].
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[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

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[1]

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[1]

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.

体内研究
(In Vivo)

NCT-58 (30 mg/kg; i.p.; every other day for 47 days) suppresses Trastuzumab-resistant tumor growth[1].
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[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Trastuzumab-resistant xenograft model (female nude mice; 6 weeks; BALB/c)[1]
Dosage: 30 mg/kg
Administration: i.p.; every other day for 47 days
Result: Significantly reduced tumor growth.

分子量

466.57

Formula

C27H34N2O5
CAS 号

2411429-33-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Park S, et al. The C-terminal HSP90 inhibitor NCT-58 kills trastuzumab-resistant breast cancer stem-like cells. Cell Death Discov. 2021;7(1):354.

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