HP590|西域试剂

HP590,98.59%

产品编号：Bellancom-151480| 分子式：C₂₉H₂₄F₆N₄O₃| 分子量：590.52

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-151480	￥3800.00	杭州北京（现货）
Bellancom-151480	￥6000.00	杭州北京（现货）
Bellancom-151480	￥11500.00	杭州北京（现货）

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HP590

产品介绍

HP590 是一种具有口服活性的、新型和强效的 STAT3 抑制剂 (STAT3 荧光素酶活性: IC₅₀=27.8 nM; ATP 抑制: IC₅₀=24.7 nM)。HP590 对胃癌细胞显示出抗增殖活性并可诱导细胞凋亡。

生物活性

HP590 is an orally active, novel and potent STAT3 inhibitor (STAT3 luciferase activity: IC₅₀=27.8 nM; ATP inhibition: IC₅₀=24.7 nM). HP590 shows anti-proliferative activity to gastric cancer cells and induces apoptosis.

体外研究

HP590 (0-40 μM; 72 h) shows anti-proliferative activities to MKN45, AGS, and MGC803 cells.
HP590 (0-40 nM; 0-24 h) inhibits STAT3 Tyr⁷⁰⁵ and Ser⁷²⁷ phosphorylation in GC cells, blocks the expression of STAT3 downstream genes (c-Myc and cyclin D1) in GC cells, reduces IL-6-mediated STAT3 nuclear translocation in MKN45 cells.
HP590 (5-20 nM; 48 h) induces gastric cancer cell apoptosis.

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

Cell Proliferation Assay

Cell Line:	MKN45, AGS, and MGC803 cells
Concentration:	0-40 μM
Incubation Time:	72 hours
Result:	Inhibited MKN45, AGS, and MGC803 cells with IC₅₀s of 9.3, 13.5, and 8.7 nM, respectively.

Apoptosis Analysis

Cell Line:	MKN45 and AGS cells
Concentration:	5, 10, and 20 nM
Incubation Time:	48 hours
Result:	Induced apoptosis in MKN45 and AGS cells in a dose-dependent manner.

Western Blot Analysis

Cell Line:	Gastric Cancer Cells
Concentration:	0-40 nM
Incubation Time:	0-24 h
Result:	Inhibited STAT3 p-Tyr⁷⁰⁵ and p-Ser⁷²⁷ in GC cells completely at 40 nM. Blocked the expression of STAT3 downstream genes, including c-Myc and cyclin D1, in a concentration-dependent and time-dependent manner. Showed the STAT3 p-Tyr⁷⁰⁵ stimulated by IL-6 in GC cell lines, but entirely suppressed by HP590 at 40 nM.

RT-PCR

Cell Line:	MKN45 and AGS cells
Concentration:	10, 20, and 40 nM
Incubation Time:	48 hours
Result:	Suppressed the expression of STAT3 downstream genes (c-Myc and cyclin D1) at the mRNA level.

体内研究
(In Vivo)

HP590 (oral administration; 25 and 50 mg/kg; once daily; 5 w) inhibits GC growth effectively by inhibiting the STAT3 activation and shows better tolerance in GC xenograft model.

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

Animal Model:	BALB/c-nude mice injected with GC cells
Dosage:	25 and 50 mg/kg
Administration:	Oral administration; 25 and 50 mg/kg; once daily; 5 weeks
Result:	Inhibited MKN45 tumor growth in a concentration-dependent manner. Inhibited STAT3 phosphorylation at Tyr705 and Ser727 and reduced the expression of the downstream genes. Inhibited the expression of Ki67 (a proliferation marker). Showed no weight loss during HP590 treatment, and no apparent damage in the major organs of mice.

体内研究

HP590 (oral administration; 25 and 50 mg/kg; once daily; 5 w) inhibits GC growth effectively by inhibiting the STAT3 activation and shows better tolerance in GC xenograft model.

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

Animal Model:	BALB/c-nude mice injected with GC cells
Dosage:	25 and 50 mg/kg
Administration:	Oral administration; 25 and 50 mg/kg; once daily; 5 weeks
Result:	Inhibited MKN45 tumor growth in a concentration-dependent manner. Inhibited STAT3 phosphorylation at Tyr705 and Ser727 and reduced the expression of the downstream genes. Inhibited the expression of Ki67 (a proliferation marker). Showed no weight loss during HP590 treatment, and no apparent damage in the major organs of mice.

体内研究

HP590 (oral administration; 25 and 50 mg/kg; once daily; 5 w) inhibits GC growth effectively by inhibiting the STAT3 activation and shows better tolerance in GC xenograft model.

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

Animal Model:	BALB/c-nude mice injected with GC cells
Dosage:	25 and 50 mg/kg
Administration:	Oral administration; 25 and 50 mg/kg; once daily; 5 weeks
Result:	Inhibited MKN45 tumor growth in a concentration-dependent manner. Inhibited STAT3 phosphorylation at Tyr705 and Ser727 and reduced the expression of the downstream genes. Inhibited the expression of Ki67 (a proliferation marker). Showed no weight loss during HP590 treatment, and no apparent damage in the major organs of mice.