CS-2124

中文名称:

CS-2124

中文同义词:

PIM激酶抑制剂(M-110)

英文名称:

2-[[3-(4-Morpholinyl)propyl]amino]-4-pyridinecarboxylic acid 2-[1-(4-chloro-2-hydroxyphenyl)propylidene]hydrazide

英文同义词:

CS-2124;2-[[3-(4-Morpholinyl)propyl]amino]-4-pyridinecarboxylic acid 2-[1-(4-chloro-2-hydroxyphenyl)propylidene]hydrazide;M-110;4-Pyridinecarboxylic acid, 2-[[3-(4-morpholinyl)propyl]amino]-, 2-[1-(4-chloro-2-hydroxyphenyl)propylidene]hydrazide;M-110 >=98% (HPLC)

CAS号:

1395048-49-3

分子式:

C22H28ClN5O3

分子量:

445.94

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

1395048-49-3.mol

密度 

1.31±0.1 g/cm3(Predicted)

储存条件 

2-8°C

溶解度 

DMSO: soluble25mg/mL, clear

形态

powder

酸度系数(pKa)

7.46±0.40(Predicted)

颜色

white to beige

CAS 数据库

1395048-49-3

生物活性

M-110 是一种高选择性的，ATP 竞争性的 PIM 激酶抑制剂，M-110 对 PIM-3 抑制作用最好，IC50=47 nM。M-110 抑制 PIM-1 和 PIM-2 的IC50 为 2.5 μM。M-110 抑制前列腺癌细胞的增殖，IC50 为 0.6-0.9 μM。

体外研究

M-110 (0.01-10 μM; 72 hours) inhibiting the growth of DU-145 cells with an IC 50 value of 0.9 μM. M-110 has no activity on normal human peripheral blood mononuclear cells up to 40 μM. M-110 (10 μM; 18 hours) inhibits STAT3 Tyr705 phosphorylation. M-110 inhibits the expression of active STAT3 through inhibition of PIM-3. M-110 also inhibits the proliferation of 22Rv1, PC3, and SW480 cells, with IC50 values of 0.6 to 0.8 μM. Cell Viability Assay Cell Line: DU-145 cells Concentration: 0.01, 0.1, 1, 10 μM Incubation Time: 72 hours Result: Inhibiting the growth of DU-145 cells with an IC 50 value of 0.9 μM. Western Blot Analysis Cell Line: DU-145 cells Concentration: 10 μM Incubation Time: 18 hours Result: Reduced the expression of p-STAT3 Tyr705 to 23.5%, compared with untreated cells without affecting the expression of STAT3.

Cell Line:

DU-145 cells

Concentration:

0.01, 0.1, 1, 10 μM

Incubation Time:

72 hours

Result:

Inhibiting the growth of DU-145 cells with an IC 50 value of 0.9 μM.

Cell Line:

DU-145 cells

Concentration:

10 μM

Incubation Time:

18 hours

Result:

Reduced the expression of p-STAT3 Tyr705 to 23.5%, compared with untreated cells without affecting the expression of STAT3.

WGK Germany 

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