1395048-49-3
中文名稱
CS-2124
英文名稱
2-[[3-(4-Morpholinyl)propyl]amino]-4-pyridinecarboxylic acid 2-[1-(4-chloro-2-hydroxyphenyl)propylidene]hydrazide
CAS
1395048-49-3
分子式
C22H28ClN5O3
分子量
445.94
MOL 文件
1395048-49-3.mol
更新日期
2023/03/20 15:41:25
1395048-49-3 結(jié)構(gòu)式
基本信息
中文別名
PIM激酶抑制劑(M-110) 英文別名
M-110CS-2124
M-110 >=98% (HPLC)
2-[[3-(4-Morpholinyl)propyl]amino]-4-pyridinecarboxylic acid 2-[1-(4-chloro-2-hydroxyphenyl)propylidene]hydrazide
4-Pyridinecarboxylic acid, 2-[[3-(4-morpholinyl)propyl]amino]-, 2-[1-(4-chloro-2-hydroxyphenyl)propylidene]hydrazide
物理化學(xué)性質(zhì)
密度1.31±0.1 g/cm3(Predicted)
儲(chǔ)存條件2-8°C
溶解度DMSO：可溶，25mg/mL，澄清
酸度系數(shù)(pKa)7.46±0.40(Predicted)
形態(tài)粉末
顏色白色至米色
常見(jiàn)問(wèn)題列表
生物活性
M-110 是一種高選擇性的，ATP 競(jìng)爭(zhēng)性的 PIM 激酶抑制劑，M-110 對(duì) PIM-3 抑制作用最好，IC50=47 nM。M-110 抑制 PIM-1 和 PIM-2 的IC50 為 2.5 μM。M-110 抑制前列腺癌細(xì)胞的增殖，IC50 為 0.6-0.9 μM。體外研究
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. |