2059952-75-7
中文名稱
STAT3-IN-1
英文名稱
STAT3-IN-1
CAS
2059952-75-7
分子式
C28H29NO6
分子量
475.53
MOL 文件
2059952-75-7.mol
更新日期
2024/12/23 09:08:09
2059952-75-7 結(jié)構(gòu)式
基本信息
中文別名
化合物STAT3-IN-1 英文別名
STAT3-IN-12-Propenamide, N-[4-[(1E)-2-(3,5-dimethoxyphenyl)ethenyl]phenyl]-3-(3,4,5-trimethoxyphenyl)-, (2E)-
物理化學(xué)性質(zhì)
沸點(diǎn)689.3±55.0 °C(Predicted)
密度1.205±0.06 g/cm3(Predicted)
儲(chǔ)存條件Sealed in dry,Room Temperature
溶解度DMSO: 125 mg/mL (262.86 mM)
酸度系數(shù)(pKa)12.63±0.70(Predicted)
形態(tài)Solid
顏色Light yellow to orange
常見(jiàn)問(wèn)題列表
生物活性
STAT3-IN-1 (compound 7d) 是一種出色的、選擇性的 STAT3 的口服活性抑制劑，在HT29細(xì)胞和MDA-MB 231細(xì)胞中的IC50值分別為1.82 μM和2.14 μM。STAT3-IN-1 誘導(dǎo)腫瘤細(xì)胞凋亡。靶點(diǎn)
| Target | Value |
|
STAT3
(in HT29 cells) | 1.82 μM |
|
STAT3
(in MDA-MB 231 cells) | 2.14 μM |
體外研究
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. |
體內(nèi)研究
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. |