1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis
  2. HSP Apoptosis
  3. 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。

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NCT-58 Chemical Structure

NCT-58 Chemical Structure

CAS No. : 2411429-33-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥4400
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1 mg ¥1600
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5 mg ¥4000
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10 mg ¥6800
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

MCE 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].

MCE 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
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 50 mg/mL (107.17 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.82%

参考文献

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1433 mL 10.7165 mL 21.4330 mL 53.5825 mL
5 mM 0.4287 mL 2.1433 mL 4.2866 mL 10.7165 mL
10 mM 0.2143 mL 1.0717 mL 2.1433 mL 5.3583 mL
15 mM 0.1429 mL 0.7144 mL 1.4289 mL 3.5722 mL
20 mM 0.1072 mL 0.5358 mL 1.0717 mL 2.6791 mL
25 mM 0.0857 mL 0.4287 mL 0.8573 mL 2.1433 mL
30 mM 0.0714 mL 0.3572 mL 0.7144 mL 1.7861 mL
40 mM 0.0536 mL 0.2679 mL 0.5358 mL 1.3396 mL
50 mM 0.0429 mL 0.2143 mL 0.4287 mL 1.0717 mL
60 mM 0.0357 mL 0.1786 mL 0.3572 mL 0.8930 mL
80 mM 0.0268 mL 0.1340 mL 0.2679 mL 0.6698 mL
100 mM 0.0214 mL 0.1072 mL 0.2143 mL 0.5358 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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