EB-3D|cas:1839150-63-8|西域试剂

EB-3D,99.54%

产品编号：Bellancom-115463| CAS NO：1839150-63-8| 分子式：C₃₀H₃₆Br₂N₄O₂| 分子量：644.44

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货号	价格	库存与货期
Bellancom-115463	￥1900.00	杭州北京（现货）
Bellancom-115463	￥3000.00	杭州北京（现货）
Bellancom-115463	￥8300.00	杭州北京（现货）

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EB-3D

产品介绍

EB-3D 是有效的选择性胆碱激酶 α (ChoKα) 抑制剂，对 ChoKα1 的 IC₅₀ 值为 1 μM。EB-3D 对 ChoKα 表达、AMPK 激活、细胞凋亡 (apoptosis)、内质网应激和脂质代谢有影响。EB-3D 在一组T-白血病细胞系中显示出强大的抗增殖活性。具有抗癌活性。

生物活性

EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC₅₀ of 1 μM for ChoKα1. EB-3D exerts effects on ChoKα expression, AMPK activation, apoptosis, endoplasmic reticulum stress and lipid metabolism. EB-3D exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines. Anti-cancer activity.

体外研究

EB-3D displays (0-100 μM; 72 hours) excellent antiproliferative activity against a wide cohort of T-leukemic cell lines, with GI GI₅₀s 13 values in the nanomolar range.
EB-3D (1.25-5μM; 24 hours) induced apoptosis in leukemia cell lines.
EB-3D (0.5-1 μM; 24 hours) induces a G0/G1 arrest that lead to apoptosis.
EB-3D (0.3 μM; 48 hours) shows a first spike of activation of AMPKα after 30 minutes and a later increase in the phosphorylation of T172.
EB-3D (1-40 μM; 48 hours) inhibits cell growth in HepG2 cells with a GI₅₀ of 14.55 μM.
EB-3D induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line:	JURKAT, CCRF-CEM, HSB-2, MOLT-16, DNA-41, LOUCY, PEER, ALL-SIL cells
Concentration:	0.001, 0.01, 0.1, 1, 10, 100 μM
Incubation Time:	72 hours
Result:	Inhibited JURKAT, CCRF-CEM, HSB-2, MOLT-16, DNA-41, LOUCY, PEER, and ALL-SIL cells growth with GI₅₀s of 136.2, 478.8, 17.7, 0.9, 60.6, 200, 265, and 132 nM, respectively.

Apoptosis Analysis

Cell Line:	Jurkat, CCRF-CEM and HSB-2 cells
Concentration:	1.25, 2.5, 5 μM
Incubation Time:	24 hours
Result:	Induced apoptosis in leukemia cell lines.

Cell Cycle Analysis

Cell Line:	Jurkat, CCRF-CEM and HSB-2 cells
Concentration:	0.5, 1 μM
Incubation Time:	24 hours
Result:	Induces cell cycle arrest in G0/G1 phase.

Western Blot Analysis

Cell Line:	Jurkat cells
Concentration:	0.3 μM
Incubation Time:	48 hours
Result:	Showed a first spike of activation of AMPKα after 30 minutes of treatment and a later increase in the phosphorylation of T172. The increase in S79 phosphorylation of its main target ACC (acetyl-coenzyme A (CoA) carboxylase), followed the same pattern. This rapid activation of AMPK, in turn induced a consequent reduction in mTOR phosphorylation that is visible already at 30’ and that becomes amplified at longer time probably due to the interruption of feedback loops that are characteristic of mTOR connecting pathways.

体内研究
(In Vivo)

EB-3D (1 mg/kg; i.p.; every other day) impairs mammary tumor growth in syngeneic orthotopic E0771-C57BL/6 mouse model^[4].
EB-3D (2.5 mg/kg; every other day for 4 weeks) shows a reduction of the number of spontaneous lung macro- and micrometastasis^[4].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	E0771-C57BL/6 mice^[4]
Dosage:	I.p.; every other day for 4 weeks
Administration:	2.5 mg/kg
Result:	A reduction of the number of spontaneous lung macro- and micrometastasis.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	E0771-C57BL/6 mice^[4]
Dosage:	I.p.; every other day for 4 weeks
Administration:	2.5 mg/kg
Result:	A reduction of the number of spontaneous lung macro- and micrometastasis.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	E0771-C57BL/6 mice^[4]
Dosage:	I.p.; every other day for 4 weeks
Administration:	2.5 mg/kg
Result:	A reduction of the number of spontaneous lung macro- and micrometastasis.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (77.59 mM; Need ultrasonic)

H₂O : ≥ 9.09 mg/mL (14.11 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	1.5517 mL	7.7587 mL	15.5173 mL
5 mM	0.3103 mL	1.5517 mL	3.1035 mL
10 mM	0.1552 mL	0.7759 mL	1.5517 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 (sealed storage, away from moisture)。-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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献