EHT 1610

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EHT 1610

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:

1425945-60-3

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品介绍

EHT 1610 是双特异性酪氨酸磷酸化调节酶 (DYRK) 的强效抑制剂，抑制DYRK1A和DYRK1B的IC₅₀分别为 0.36 nM 和 0.59 nM。EHT 1610 具有抗白血病的作用，并能够调节细胞周期，诱导细胞凋亡 (apoptosis)。

生物活性

EHT 1610 is a potent inhibitor ofDYRK, withIC₅₀sof 0.36 nM (DYRK1A), 0.59 nM (DYRK1B), respectively. EHT 1610 exhibits antileukemia effect, regulates cell cycle and induces cellapoptosis^[1]^-^[4].

IC₅₀& Target

IC50: 0.36 nM (DYRK1A), 0.59 nM (DYRK1B)^[1]

体外研究
(In Vitro)

EHT 1610 induces apoptosis of primary ALL cells that were resistant to cytarabine^[2].
EHT 1610 dose-dependently induces apoptosis in B- and T-cell lines and primary human pediatric^[2].
EHT 1610 (; 72 h) inhibits DYRK1A, results loss of DYRK1A-mediated FOXO1 and STAT3 signaling, leading to preferential cell death in leukemic B cells^[3].
EHT 1610 (2.5-10 μM; 4-5 h) inhibits phosphorylation of FOXO1, STAT3 and cyclin D3, thus regulates late cell-cycle progression, mitochondrial ROS and DNA damage, respectively^[3].

Western Blot Analysis^[3]

Cell Line:	MHH-CALL-4 cells
Concentration:	0, 2.5, 5, 10 μM
Incubation Time:	4, 5 hours
Result:	Reduced p-cyclin D3 (Thr283), and p-FOXO1 protein level in a dose-dependent manner.

体内研究
(In Vivo)

EHT 1610 (20 mg/kg/d; i.p.; twice a day; 3 weeks) shows antileukemia activity against in leukemic aggressive model in mice^[3].

Animal Model:	Xenograft models of B-ALL in mice (12-14 weeks old)^[3]
Dosage:	20 mg/kg
Administration:	Intraperitoneal injection; twice a day, 5 days on, 2 days off; 3 weeks
Result:	Reduced leukemic burden by approximately 8% and conferred a modest survival advantage.

分子量

383.40

性状

Solid

Formula

C₁₈H₁₄FN₅O₂S

CAS 号

1425945-60-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。

溶解性数据

In Vitro:

DMSO : 5 mg/mL(13.04 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.6082 mL	13.0412 mL	26.0824 mL
5 mM	0.5216 mL	2.6082 mL	5.2165 mL
10 mM	0.2608 mL	1.3041 mL	2.6082 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；该产品在溶液状态不稳定，建议您现用现配，即刻使用。