NCT-58|cas:2411429-33-7|西域试剂

NCT-58,99.82%

产品编号：Bellancom-145102| CAS NO：2411429-33-7| 分子式：C₂₇H₃₄N₂O₅| 分子量：466.57

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货号	价格	库存与货期
Bellancom-145102	￥4000.00	杭州北京（现货）
Bellancom-145102	￥6800.00	杭州北京（现货）
Bellancom-145102	￥14500.00	杭州北京（现货）

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NCT-58

产品介绍

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。

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(In Vivo)

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.

西域 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)
Dosage:	30 mg/kg
Administration:	i.p.; every other day for 47 days
Result:	Significantly reduced tumor growth.

体内研究

西域 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)
Dosage:	30 mg/kg
Administration:	i.p.; every other day for 47 days
Result:	Significantly reduced tumor growth.

体内研究

西域 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)
Dosage:	30 mg/kg
Administration:	i.p.; every other day for 47 days
Result:	Significantly reduced tumor growth.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (107.17 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1433 mL	10.7165 mL	21.4330 mL
5 mM	0.4287 mL	2.1433 mL	4.2866 mL
10 mM	0.2143 mL	1.0717 mL	2.1433 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式