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  2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis
  3. HSP Apoptosis
  4. NCT-58

NCT-58是 HSP90 C末端的有效抑制劑。NCT-58 不誘導(dǎo)熱休克反應(yīng) (HSR)，因?yàn)樗邢?C 末端區(qū)域，并通過(guò)同時(shí)下調(diào) HER 家族成員以及抑制 Akt 磷酸化來(lái)引發(fā)抗腫瘤活性。NCT-58 可殺死曲妥珠單抗耐藥 (Trastuzumab-resistant) 的乳腺癌干細(xì)胞樣細(xì)胞。NCT-58 誘導(dǎo) HER2 陽(yáng)性乳腺癌細(xì)胞凋亡。在抗曲妥珠單抗異種移植模型中，NCT-58 可抑制生長(zhǎng)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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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥4400
In-stock
5 mg ￥1600
In-stock
10 mg ￥2600
In-stock
25 mg ￥5500
In-stock
50 mg 現(xiàn)貨 詢價(jià)
100 mg   詢價(jià)  
200 mg   詢價(jià)  

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Customer Review

查看 HSP 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
BT-474 IC50
8.53 μM
Compound: 80
Cytotoxicity against human BT-474 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
Cytotoxicity against human BT-474 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
[PMID: 32738983]
JIMT-1 IC50
4.45 μM
Compound: 80
Cytotoxicity against human JIMT-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
Cytotoxicity against human JIMT-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
[PMID: 32738983]
SK-BR-3 IC50
2 μM
Compound: 27; NCT-58
Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTS proliferation assay
Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTS proliferation assay
[PMID: 36549397]
體外研究
(In Vitro)

NCT-58 處理 (0.1-20 μM；72 小時(shí)) 以劑量依賴性方式降低 HER2 陽(yáng)性 BT474 和 SKBR3 細(xì)胞的細(xì)胞活力[1]。
NCT-58 處理 (0.1-10 μM；72 小時(shí)) 增加 HER2 陽(yáng)性 BT474 和 SKBR3 細(xì)胞中早期和晚期凋亡細(xì)胞的數(shù)量[1]。
NCT -58 處理 (2-10 μM；72 小時(shí)) 有效降低了 JIMT-1 和 MDA-MB-453 細(xì)胞中截短的 p95HER2 及其磷酸化形式的水平，以及 Akt 和磷酸化 Akt (Ser473) 蛋白含量的下調(diào)[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.
體內(nèi)研究
(In Vivo)

NCT-58 (30 mg/kg；腹腔注射；每隔一天，持續(xù) 47 天) 抑制曲妥珠單抗耐藥腫瘤的生長(zhǎng)[1]。
NCT-58 (30 mg/kg；腹腔注射；每隔一天，持續(xù) 47 天) 導(dǎo)致腫瘤生長(zhǎng)明顯受阻，腫瘤重量顯著下降[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 號(hào)
性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 50 mg/mL (107.17 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.82%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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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產(chǎn)品名稱：
NCT-58
目錄號(hào)：
HY-145102
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