EC359 - CAS:2012591-09-0

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EC359

目录号 : KM6951 CAS No. : 2012591-09-0 纯度 : 98%

Data Sheet 产品使用指南

EC359 是一种有效的，选择性的，高亲和力的和口服的生物利用度白血病抑制因子受体 (LIFR) 抑制剂，其 K_d 值为 10.2 nM，可直接与 LIFR 相互作用以有效阻断 LIF/LIFR 相互作用。

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10mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

EC359 is a potent, selective, high affinity and orally active leukemia inhibitory factor receptor (LIFR) inhibitor with a K_d of 10.2 nM, which directly interacts with LIFR to effectively block LIF/LIFR interactions.

体外研究

EC359 (0-100 nM; 3 days; BT-549, SUM-159, MDA-MB-231, MDA-MB-468, and HCC1806 cells) treatment reduces cell viability in a dose-dependent manner.
EC359 (20 nM, 25 nM; 72 hours; MDA-MB-231 and BT-549 cells) treatment significantly increases caspase-3/7 activity and Annexin V-positive cells in both MDAMB-231 and BT-549 cells. EC359 exhibits significant inhibitory activity on invasion and promotes apoptosis of TNBC cells.
EC359 (100 nM; 12 hours; BT549 cells) treatment significantly reduces the expression of several (such as STAT1 TGFB1, JUNB, MCL-1, etc) known STAT3 target genes.
EC359(100 nM; 1 hour; MDA-MB-231 and BT-549 cells) treatment substantially reduces the LIF activation of STAT3, also reduces the STAT3 activation by OSM and CNTF. EC359 treatment substantially decreases the phosphorylation of AKT, mTOR, S6, and ERK1/2 in MDA-MB231 and BT-549 cells. EC359 treatment also increases the phosphorylation of proapoptotic p38MAPK in BT549 cells.

Cell Viability Assay

Cell Line:	BT-549, SUM-159, MDA-MB-231, MDA-MB-468, and HCC1806 cells
Concentration:	0 nM, 1.5 nM, 12.5 nM, 25 nM, 50 nM, 100 nM
Incubation Time:	3 days
Result:	Reduced cell viability in a dose-dependent manner.

Apoptosis Analysis

Cell Line:	MDA-MB-231 and BT-549 cells
Concentration:	20 nM, 25 nM
Incubation Time:	72 hours
Result:	Promoted apoptosis of TNBC cells.

RT-PCR

Cell Line:	BT549 cells
Concentration:	100 nM
Incubation Time:	12 hours
Result:	Reduced the expression of several known STAT3 target genes.

Western Blot Analysis

Cell Line:	MDA-MB-231 and BT-549 cells
Concentration:	100 nM
Incubation Time:	1 hour
Result:	Substantially reduced the LIF activation of STAT3, reduced the STAT3 activation by OSM and CNTF, decreased the phosphorylation of AKT, mTOR, S6, and ERK1/2 in both BT-549 and MDA-MB-231 cells and increased the phosphorylation of proapoptotic p38MAPK in BT549 cells.

体内研究

EC359 (5 mg/kg; subcutaneous injection; 3 days per week; for 25 days; female athymic nude mice) treatment significantly reduces the tumor progression. The body weights of mice in EC359-treated groups remains unchanged confirming the low toxicity of EC359.

Animal Model:	8-week-old female athymic nude mice with MDA-MB-231 cells
Dosage:	5 mg/kg
Administration:	Subcutaneous injection; 3 days per week; for 25 days
Result:	Significantly reduced the tumor progression.

分子式

C₃₆H₃₈F₂O₂

分子量

540.68

CAS号

2012591-09-0

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 (231.19 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8495 mL	9.2476 mL	18.4952 mL
5 mM	0.3699 mL	1.8495 mL	3.6990 mL
10 mM	0.1850 mL	0.9248 mL	1.8495 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: ≥ 2.08 mg/mL (3.85 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.85 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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。
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.85 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.85 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。