STAT3-IN-1

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STAT3-IN-1

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2059952-75-7

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品介绍

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。

生物活性

STAT3-IN-1 (compound 7d) is an excellent, selective and orally activeSTAT3inhibitor, withIC₅₀values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor cellsapoptosis^[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].

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].

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

性状

Solid

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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本网站选购。