STAT3-IN-1

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STAT3-IN-1  纯度: 96.54%

STAT3-IN-1 (compound 7d) 是强效的、选择性的、口服有效的STAT3 的抑制剂，其在HT29 和MDA-MB 231 细胞中的 IC50 值分别为1.82 μM 和2.14 μM。STAT3-IN-1 (compound 7d) 可诱导肿瘤细胞凋亡。

STAT3-IN-1

STAT3-IN-1 Chemical Structure

CAS No. : 2059952-75-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1570 In-stock
5 mg ￥1500 In-stock
10 mg ￥2400 In-stock
50 mg ￥6800 In-stock
100 mg ￥9800 In-stock
200 mg   询价  
500 mg   询价  

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STAT3-IN-1 相关产品

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生物活性

STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor apoptosis[1].

IC50 & Target[1]

Stat-3

1.82 μM (IC50, in HT29 cells)

Stat-3

2.14 μM (IC50, in MDA-MB 231 cells)

体外研究
(In Vitro)

STAT3-IN-1 (compound 7d: 0-10 μM, 48 h) inhibits the STAT3 acetylation at lysine 685 and affected its specific genes expressions[1].
STAT3-IN-1 (compound 7d: 0-10 μM, 48 h) induces tumor cells apoptosis in MDA-MB-231 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.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cell lines.
Concentration: 0-10 μM.
Incubation Time: 48 hours.
Result: The induced apoptosis rates (early and late apoptosis) at 1, 2, 5, 8 and 10 μM were 9.0%, 11.2%, 20.9%, 43.3% and 85.2% versus control 3.0%.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 and HT-29 cell lines.
Concentration: 0-10 μM.
Incubation Time: 48 hours.
Result: Inhibited STAT3 acetylation and STAT3 tyrosine phosphorylation in MDA-MB-231 cells.
Increased the expressions of these tumor-suppressor genes (PTPN6 (SHP-1), CDKN2A and DLEC1) which were related to STAT3 acetylation at Lys685.

体内研究
(In Vivo)

STAT3-IN-1 (compound 7d: 10, 20 mg/kg, two weeks) arrests tumor growth with low toxicity in mouse-xenograft model[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: Mouse-xenograft model bearing inoculation of mice breast cancer 4T1 cells[1].
Dosage: 10, 20 mg/kg.
Administration: Oral administration once every other day for two weeks.
Result: Arrested tumor growth with no obvious body weight loss.

分子量

475.53

Formula

C28H29NO6
CAS 号

2059952-75-7
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 : 125 mg/mL (262.86 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1029 mL 10.5146 mL 21.0292 mL
5 mM 0.4206 mL 2.1029 mL 4.2058 mL
10 mM 0.2103 mL 1.0515 mL 2.1029 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: 6.25 mg/mL (13.14 mM); Suspended solution; Need ultrasonic

    此方案可获得 6.25 mg/mL (13.14 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 62.5 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]. Li S, et al. Discovery of oral-available resveratrol-caffeic acid based hybrids inhibiting acetylated and phosphorylated STAT3 protein. Eur J Med Chem. 2016 Nov 29;124:1006-1018.

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