STAT3-IN-1
| 中文名称 | STAT3-IN-1 |
|---|---|
| 中文同义词 | 化合物STAT3-IN-1;(E)-N-(4-((E)-3,5-二甲氧基苯乙烯基)苯基)-3-(3,4,5-三甲氧基苯基)丙烯酰胺 |
| 英文名称 | STAT3-IN-1 |
| 英文同义词 | STAT3-IN-1;2-Propenamide, N-[4-[(1E)-2-(3,5-dimethoxyphenyl)ethenyl]phenyl]-3-(3,4,5-trimethoxyphenyl)-, (2E)-;(E)-N-(4-((E)-3,5-Dimethoxystyryl)phenyl)-3-(3,4,5-trimethoxyphenyl)acrylamide;Inhibitor,STAT-3-IN-1,Apoptosis,inhibit,STAT3IN1,STAT,STAT3 IN 1 |
| CAS号 | 2059952-75-7 |
| 分子式 | C28H29NO6 |
| 分子量 | 475.53 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 2059952-75-7.mol |
| 结构式 |  |
STAT3-IN-1 性质
| 沸点 | 689.3±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.205±0.06 g/cm3(Predicted) |
| 储存条件 | Sealed in dry,Room Temperature |
| 溶解度 | 二甲基亚砜：125 mg/mL（262.86 mM） |
| 酸度系数(pKa) | 12.63±0.70(Predicted) |
STAT3-IN-1 (compound 7d) 是一种出色的、选择性的 STAT3 的口服活性抑制剂，在HT29细胞和MDA-MB 231细胞中的IC50值分别为1.82 μM和2.14 μM。STAT3-IN-1 诱导肿瘤细胞凋亡。
| Target | Value |
|
STAT3
(in HT29 cells) | 1.82 μM |
|
STAT3
(in MDA-MB 231 cells) | 2.14 μM |
STAT3-IN-1 (compound 7d: 0-10 μM, 48 h) inhibits the STAT3 acetylation at lysine 685 and affected its specific genes expressions.
STAT3-IN-1 (compound 7d: 0-10 μM, 48 h) induces tumor cells apoptosis in MDA-MB-231 cells.
Apoptosis Analysis
| Cell Line: | MDA-MB-231 cell lines. |
| Concentration: | 0-10 μM. |
| Incubation Time: | 48 hours. |
| Result: | The induced apoptosis rates (early and late apoptosis) at 1, 2, 5, 8 and 10 μM were 9.0%, 11.2%, 20.9%, 43.3% and 85.2% versus control 3.0%. |
Western Blot Analysis
| Cell Line: | MDA-MB-231 and HT-29 cell lines. |
| Concentration: | 0-10 μM. |
| Incubation Time: | 48 hours. |
| Result: |
Inhibited STAT3 acetylation and STAT3 tyrosine phosphorylation in MDA-MB-231 cells.
Increased the expressions of these tumor-suppressor genes (PTPN6 (SHP-1), CDKN2A and DLEC1) which were related to STAT3 acetylation at Lys685. |
STAT3-IN-1 (compound 7d: 10, 20 mg/kg, two weeks) arrests tumor growth with low toxicity in mouse-xenograft model.
| Animal Model: | Mouse-xenograft model bearing inoculation of mice breast cancer 4T1 cells. |
| Dosage: | 10, 20 mg/kg. |
| Administration: | Oral administration once every other day for two weeks. |
| Result: | Arrested tumor growth with no obvious body weight loss. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-100753 | STAT3-IN-1 | 1 mg | 681元 | |
| 2024/04/30 | S0818 | STAT3-IN-1 STAT3-IN-1 | 2059952-75-7 | 5mg | 1470元 |