NCGC00378430

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。

NCGC00378430  纯度: 99.76%

NCGC00378430 是一种有效的 SIX1/EYA2 相互作用抑制剂。NCGC00378430 部分逆转 SIX1 过表达介导的转录和代谢谱,并逆转 SIX1 诱导的 TGF-β 信号传导和上皮-间质转化 (EMT)。NCGC00378430 在小鼠模型中抑制 SIX1 介导的乳腺癌转移。

NCGC00378430

NCGC00378430 Chemical Structure

CAS No. : 920650-00-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2750 In-stock
5 mg ¥2500 In-stock
10 mg ¥4000 In-stock
25 mg ¥8500 In-stock
50 mg ¥13500 In-stock
100 mg ¥19500 In-stock
200 mg   询价  
500 mg   询价  

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NCGC00378430 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Anti-Breast Cancer Compound Library
  • Phosphatase Inhibitor Library

生物活性

NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor. NCGC00378430 partially reverses transcriptional and metabolic profiles mediated by SIX1 overexpression and reverses SIX1-induced TGF-β signaling and epithelial-mesenchymal transition (EMT). NCGC00378430 inhibits SIX1-mediated breast cancer metastasis in a mouse model[1].

体外研究
(In Vitro)

NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor with an IC50 of 52 μM in the Alphascreen assay[1].
NCGC00378430 (20 μM; 3 days) blocks TGF-β induced activation of p-Smad3, upregulation of FN1, and downregulation of E-CAD in T47D cells[1].
NCGC00378430 (10 μM; 3 days) reverses the Sine oculis homeobox homolog 1 (SIX1)-induced increase in p-SMAD3 and does not alter total E-CAD levels. NCGC00378430 restores membranous E-CAD in MCF7-SIX1 cells, along with inhibiting FN1 expression[1].
NCGC00378430 (10 or 20 μM) disrupts SIX1-EYA2 interaction in breast cancer cells (MCF7, T47D, MDA-MB-231 cells)[1].
NCGC00378430 (10 μM; for 3 days) partially reverses SIX1-mediated transcriptional and metabolic signatures in MCF7 breast tumor cells[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.

Western Blot Analysis[1]

Cell Line: T47D cells
Concentration: 20 μM
Incubation Time: 3 days
Result: Blocked TGF-β induced activation of p-Smad3, upregulation of FN1, and downregulation of E-CAD.

体内研究
(In Vivo)

NCGC00378430 (25 mg/kg; local injection to the site of tumor; every other day; from day 3 until the day 21) dramatically decreases distant metastatic burden compared to vehicle treatment[1].
NCGC00378430 (20 mg/kg; IV) has a T1/2α of 0.25 hours[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.

Animal Model: 6-8 week old NSG mice with MCF7 tumor cells[1]
Dosage: 25 mg/kg
Administration: Local Injection to the site of tumor; every other day; from day 3 until the day 21
Result: Dramatically decreased distant metastatic burden compared to vehicle treatment.
Had no growth inhibitory effect.
Animal Model: Mice[1]
Dosage: 20 mg/kg (Pharmacokinetic Analysis)
Administration: IV
Result: Had a T1/2α of 0.25 hours, a CL of 6.19 L/hr•kg, a Vss of 4.08 L/kg, a Cmax of 6703 ng/mL and an AUC of 3234 ng/mL•hr.

分子量

441.50

Formula

C22H23N3O5S

CAS 号

920650-00-6

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 : 100 mg/mL (226.50 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2650 mL 11.3250 mL 22.6501 mL
5 mM 0.4530 mL 2.2650 mL 4.5300 mL
10 mM 0.2265 mL 1.1325 mL 2.2650 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 (5.66 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.66 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

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.66 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*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]. Hengbo Zhou, et al. Identification of a Small-Molecule Inhibitor That Disrupts the SIX1/EYA2 Complex, EMT, and Metastasis. Cancer Res. 2020 Jun 15;80(12):2689-2702.

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