STAT3-IN-1
|
|
|
- CAS号:
- 2059952-75-7
- 英文名:
- STAT3-IN-1
- 英文别名:
- STAT3-IN-1;Inhibitor,STAT-3-IN-1,Apoptosis,inhibit,STAT3IN1,STAT,STAT3 IN 1;(E)-N-(4-((E)-3,5-Dimethoxystyryl)phenyl)-3-(3,4,5-trimethoxyphenyl)acrylamide;2-Propenamide, N-[4-[(1E)-2-(3,5-dimethoxyphenyl)ethenyl]phenyl]-3-(3,4,5-trimethoxyphenyl)-, (2E)-
- 中文名:
- STAT3-IN-1
- 中文别名:
- 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
- CBNumber:
- CB15821188
- 分子式:
- C28H29NO6
- 分子量:
- 475.53
- MOL File:
- 2059952-75-7.mol
|
|
|
STAT3-IN-1化学性质
-
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:
-
DMSO: 125 mg/mL (262.86 mM)
-
|
-
酸度系数(pKa):
-
12.63±0.70(Predicted)
-
|
-
形态:
-
Solid
-
|
-
颜色:
-
Light yellow to orange
-
|
STAT3-IN-1性质、用途与生产工艺
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.
|
STAT3-IN-1
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/08/19 | HY-100753 | STAT3-IN-1 | | 1 mg | 681元 |
| 2024/08/19 | HY-100753 | STAT3-IN-1
STAT3-IN-1 | 2059952-75-7 | 5mg | 1500元 |
2059952-75-7, STAT3-IN-1 相关搜索:
- 抑制剂
- 药靶配体
- (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
- 化合物STAT3-IN-1
- 2059952-75-7
- Inhibitor,STAT-3-IN-1,Apoptosis,inhibit,STAT3IN1,STAT,STAT3 IN 1
- (E)-N-(4-((E)-3,5-Dimethoxystyryl)phenyl)-3-(3,4,5-trimethoxyphenyl)acrylamide
- 2-Propenamide, N-[4-[(1E)-2-(3,5-dimethoxyphenyl)ethenyl]phenyl]-3-(3,4,5-trimethoxyphenyl)-, (2E)-
- STAT3-IN-1