EHT 1610|cas:1425945-60-3|西域试剂

EHT 1610

产品编号：Bellancom-111380| CAS NO：1425945-60-3| 分子式：C₁₈H₁₄FN₅O₂S| 分子量：383.40

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货号	价格	库存与货期
Bellancom-111380	￥4500.00	杭州北京（现货）
Bellancom-111380	￥8000.00	杭州北京（现货）
Bellancom-111380	￥16500.00	杭州北京（现货）
Bellancom-111380	￥25500.00	杭州北京（现货）
Bellancom-111380	￥38000.00	杭州北京（现货）

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EHT 1610

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 of DYRK, with IC₅₀s of 0.36 nM (DYRK1A), 0.59 nM (DYRK1B), respectively. EHT 1610 exhibits antileukemia effect, regulates cell cycle and induces cell apoptosis^-^[4].

体外研究

EHT 1610 induces apoptosis of primary ALL cells that were resistant to cytarabine.
EHT 1610 dose-dependently induces apoptosis in B- and T-cell lines and primary human pediatric.
EHT 1610 (; 72 h) inhibits DYRK1A, results loss of DYRK1A-mediated FOXO1 and STAT3 signaling, leading to preferential cell death in leukemic B cells.
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.

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

Western Blot Analysis

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.

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

Animal Model:	Xenograft models of B-ALL in mice (12-14 weeks old)
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.

体内研究

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

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

Animal Model:	Xenograft models of B-ALL in mice (12-14 weeks old)
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.

体内研究

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

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

Animal Model:	Xenograft models of B-ALL in mice (12-14 weeks old)
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.