Mps1-IN-5

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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 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.