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Mps1-IN-5
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。
Mps1-IN-5图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
Mps1-IN-5 是一种有效的,具有口服活性的Mps1抑制剂,IC50值为 29 nM。Mps1-IN-5 诱导细胞凋亡 (apoptosis) 和胞周期停滞在 G2/M 期。Mps1-IN-5 显示出抗增殖活性和抗肿瘤活性。Mps1-IN-5 抑制 Mps1 的磷酸化并诱导 DNA 损伤。
生物活性

Mps1-IN-5 is a potent and orally activeMps1inhibitor with anIC50value of 29 nM. Mps1-IN-5 inducesapoptosisand cell cycle arrests at G2/M phase. Mps1-IN-5 shows antiproliferative activity and anti-tumor activity. Mps1-IN-5 inhibits phosphorylation ofMps1and induces DNA damage[1].

IC50& Target

IC50: 29 nM (Mps1)[1]

体外研究
(In Vitro)

Mps1-IN-5 (compound 12) (0-10 μM,24, 48, 72 h) 以时间依赖性方式抑制 MCF-7 和 4T1 细胞的增殖[1].< br/>Mps1-IN-5 (0, 0.5, 1.0, 5.0 μM; 24, 48 h) 在 MCF-7 和 4T1 细胞中以剂量依赖性方式诱导细胞凋亡和胞周期停滞在 G2/M 期[1].
Mps1-IN-5 (0, 0.03, 0.1, 1, 3 μM; 2 h) 抑制 Mps1 的磷酸化并诱导 DNA 损伤[1]

Cell Proliferation Assay[1]

Cell Line:MDA-MB-231, MCF-7, 4T1, HEY, OVCAR-3, ES-2, HCT-116, A549, AGS cells
Concentration:0-3 μM
Incubation Time:72 h
Result:Inhibited the cell growth with IC50s of 2.68, 0.37, 0.40, >3, >3, >3, 1.06, 2.03, >3 μM for MDA-MB-231, MCF-7, 4T1, HEY, OVCAR-3, ES-2, HCT-116, A549, AGS cells, respectively.

Cell Cycle Analysis[1]

Cell Line:MCF-7, 4T1 cells
Concentration:0, 0.5, 1.0, 5.0 μM
Incubation Time:24 h
Result:Induced cell cycle arrest of MCF-7 and 4T1 cells at the G2/M phase in a dose-dependent manner, decreased the protein expression levels of Cyclin B1 and CDK1.

Apoptosis Analysis[1]

Cell Line:MCF-7, 4T1 cells
Concentration:0, 0.5, 1.0, 5.0 μM
Incubation Time:48 h
Result:Induced apoptosis and significantly increased the expression level of an apoptosis-related protein, cleaved poly ADP-ribose polymerase (PARP).

Western Blot Analysis[1]

Cell Line:MCF-7, 4T1 cells
Concentration:0, 0.03, 0.1, 1, 3 μM
Incubation Time:2 h
Result:Increased the expression of level of γ-H2AX protein and decreased the protein expression of p-Mps1 in a dose-dependent manner.
体内研究
(In Vivo)

Mps1-IN-5 (30, 60 mg/kg; p.o.; daily for 15 days) 在乳腺癌模型中抑制肿瘤生长而无明显毒性[1]

Animal Model:6-8 weeks, female BALB/C mice (4T1-luc mouse xenograft model)[1]
Dosage:30, 60 mg/kg
Administration:P.o.; daily for 15 days
Result:Significantly suppressed tumor growth and caused negligible damage to organs such as heart, liver, spleen, lung and kidneys.
分子量

439.52

Formula

C24H25N9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.