iCRT 14

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iCRT 14  纯度: 99.84%

iCRT 14 是一种 β-连环蛋白应答转录(CRT)抑制剂,能够抑制 Wnt 信号通路,IC50 值为 40.3 nM。

iCRT 14

iCRT 14 Chemical Structure

CAS No. : 677331-12-3

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥968 In-stock
5 mg ¥880 In-stock
10 mg ¥1400 In-stock
50 mg ¥5910 In-stock
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iCRT 14 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
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  • Wnt/Hedgehog/Notch Compound Library
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  • Cytoskeleton Compound Library
  • Neuroprotective Compound Library
  • Anti-Breast Cancer Compound Library
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  • Anti-Colorectal Cancer Compound Library

生物活性

iCRT 14 is a novel potent inhibitor of β-catenin-responsive transcription (CRT), with IC50 of 40.3 nM against Wnt responsive STF16 luciferase.

IC50 & Target

IC50: 40.3 nM (Wnt responsive STF16 luciferase)[1]

体外研究
(In Vitro)

iCRT14 can interfere with TCF binding to DNA in addition to its ability to influence TCF-β-cat interaction[1]. iCRT14 (10, 25, 50 μM) effectively inhibits cell proliferation in BT-549 cells in a dose- and time-dependent manner, but still less potent than iCRT3[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

iCRT14 (50 mg/kg, i.p.) markedly decreases CycD1, proliferation of the tumors in HCT116 xenografts[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

375.44

Formula

C21H17N3O2S

CAS 号

677331-12-3

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 : ≥ 29 mg/mL (77.24 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6635 mL 13.3177 mL 26.6354 mL
5 mM 0.5327 mL 2.6635 mL 5.3271 mL
10 mM 0.2664 mL 1.3318 mL 2.6635 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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.66 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.66 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Gonsalves FC, et al. An RNAi-based chemical genetic screen identifies three small-molecule inhibitors of the Wnt/wingless signaling pathway. Proc Natl Acad Sci USA. 2011 Apr 12;108(15):5954-63.

    [2]. Bilir B, et al. Wnt signaling blockage inhibits cell proliferation and migration, and induces apoptosis in triple-negative breast cancer cells. J Transl Med. 2013 Nov 4;11:280.

Cell Assay
[2]

Cells are seeded at 20,000 cells/well into 96-well plates. After overnight incubation, cells are treated with DMSO or each Wnt inhibitor (iCRT-3, 75 μM; iCRT-5, 200 μM; iCRT-14, 50 μM; IWP-4, 5 μM and XAV-939, 10 μM) for 48 hours. Cell viability is determined using the Cell Titer-Glo luminescent cell viability assay kit. Luminescence is measured using FLUOstar microplate reader. All treatments are performed in triplicate, and each experiment is repeated three times.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Gonsalves FC, et al. An RNAi-based chemical genetic screen identifies three small-molecule inhibitors of the Wnt/wingless signaling pathway. Proc Natl Acad Sci USA. 2011 Apr 12;108(15):5954-63.

    [2]. Bilir B, et al. Wnt signaling blockage inhibits cell proliferation and migration, and induces apoptosis in triple-negative breast cancer cells. J Transl Med. 2013 Nov 4;11:280.

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