EB-3D|1839150-63-8|-陌孚医药/Medlife

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EB-3D

目录号: PL02256 纯度: ≥99%

CAS No. :1839150-63-8

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中文名称	EB-3D
英文名称	EB-3D
英文别名	EB-3D;1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-(dimethylamino)pyridinium) bromide;1-[[4-[2-[4-[[4-(Dimethylamino)pyridin-1-ium-1-yl]methyl]phenoxy]ethoxy]phenyl]methyl]-N,N-dimethylp
Cas No.	1839150-63-8
分子式	C₃₀H₃₆Br₂N₄O₂
分子量	644.44
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	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 IC 50 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.
性状	Solid
IC50 & Target[1][2]	IC50: 1 μM; Kd: 0.7 μM
体外研究(In Vitro)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
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. EB-3D (2.5 mg/kg; every other day for 4 weeks) shows a reduction of the number of spontaneous lung macro- and micrometastasis. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Mariotto E, et al. EB-3D a novel choline kinase inhibitor induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells. Biochem Pharmacol. 2018 Sep;155:213-223. [2]. Sola-Leyva A, et al. Choline kinase inhibitors EB-3D and EB-3P interferes with lipid homeostasis in HepG2 cells. Sci Rep. 2019 Mar 25;9(1):5109.

溶解度数据	In Vitro: DMSO : 50 mg/mL (77.59 mM; Need ultrasonic)H₂O : ≥ 9.09 mg/mL (14.11 mM)

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