2111834-61-6
中文名稱
STAT5-IN-2
英文名稱
STAT5-IN-2
CAS
2111834-61-6
分子式
C26 H27 N3 O
分子量
397.51
MOL 文件
2111834-61-6.mol
2111834-61-6 結構式
基本信息
中文別名
BUN34616化合物 T16940
化合物STAT5-IN-2
英文別名
STAT5-IN-2STAT5 inhibitor 17f
Quinoline, 1,2,3,4-tetrahydro-1-[2-(1H-indol-5-yloxy)ethyl]-4,4-dimethyl-6-(3-pyridinyl)-
物理化學性質
沸點635.5±55.0 °C(Predicted)
密度1.160±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO : 100 mg/mL (251.57 mM; Need ultrasonic)
酸度系數(pKa)16.56±0.30(Predicted)
形態(tài)Solid
顏色Off-white to light yellow
常見問題列表
生物活性
STAT5-IN-2 是 STAT5 的抑制劑，在 K562 和 KU812 細胞中的 EC50 分別為 9 μM和 5 μM，在文獻 1 的名稱是 17f。STAT5-IN-2 具有高效的抗白血病活性。靶點
|
STAT5 9 μM (EC 50 , in K562 cells) |
STAT5 5 μM (EC 50 , in KU812 cells ) |
體外研究
STAT5-IN-2 has EC
50
values of 9 μM and 5 μM in K562 and KU812 cells, respectively.
STAT5-IN-2 (100 nM-50 μM; 48 hours) has EC
50
values of 2.6 μM and 3.5 μM in KG1a and MV-4-11 cells, respectively.
STAT5-IN-2 (10 μM; 48 hours) induces apoptosis in all cell lines (K562, KU812, KG1a and MV-4-11 cells).
STAT5-IN-2 (10 μM; 24 hours) blocks phosphorylation of STAT5.
Cell Viability Assay
| Cell Line: | KG1a and MV-4-11 cell lines |
| Concentration: | 100 nM, 10 μM, 20 μM, 30 μM, 40 μM, 50 μM |
| Incubation Time: | 48 hours |
| Result: | Inhibited cell growth in KG1a and MV-4-11 cell lines |
Apoptosis Analysis
| Cell Line: | K562, KU812, KG1a and MV-4-11 cells |
| Concentration: | 10 μM |
| Incubation Time: | 48 hours |
| Result: | Significantly increased the number of apoptotic cells. |
Western Blot Analysis
| Cell Line: | KG1a, MV-4-11 and KU812 cells |
| Concentration: | 10 μM |
| Incubation Time: | 24 hours |
| Result: | Inhibited phosphorylation of STAT5 compared to no influence on phosphorylation level of STAT3, Akt and Erk1/2. |