SC-43
| 中文名称 | SC-43 |
|---|---|
| 中文同义词 | 化合物SC-43;1-(4-氯-3-(三氟甲基)苯基)-3-(3-(4-氰基苯氧基)苯基)脲 |
| 英文名称 | SC-43 |
| 英文同义词 | 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(3-(4-cyanophenoxy)phenyl)urea;SC-43;Urea, N-[4-chloro-3-(trifluoromethyl)phenyl]-N'-[3-(4-cyanophenoxy)phenyl]-;antiproliferative,Inhibitor,SC-43,SHP-1,PTPN6,Phosphatase,Apoptosis,caspase-3,SC 43,anti-fibrotic,p-STAT3,anticancer,orally,SC43,PARP,STAT,inhibit |
| CAS号 | 1400989-25-4 |
| 分子式 | C21H13ClF3N3O2 |
| 分子量 | 431.8 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1400989-25-4.mol |
| 结构式 |  |
SC-43 性质
| 沸点 | 462.0±45.0 °C(Predicted) |
|---|---|
| 密度 | 1.46±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 二甲基亚砜：250 mg/ml（578.97 mM） |
| 形态 | 固体 |
| 酸度系数(pKa) | 12.92±0.70(Predicted) |
| Target | Value |
|
SHP-1
() | |
|
STAT3
() |
SC-43 (0-10 μM; 24-72 hours; HuCCT-1, KKU-100, and CGCCA cells) treatment reveals the anti-proliferative effects in cholangiocarcinoma (CCA) cell lines in a dose-dependent manner after treating 24, 48 and 72 hours respectively.
SC-43 (0-10 μM; 24 hours; HuCCT-1, KKU-100, and CGCCA cells) treatment shows increased sub-G1 cells and G2-M arrest, indicating SC-43 induced differential apoptotic effects in these cell lines.
SC-43 (0-10 μM; 24 hours; HuCCT-1, KKU-100, and CGCCA cells) treatment demonstrates significant increase in cleaved caspase-3 and PARP level.
SC-43 activates SH2 domain-containing phosphatase 1 (SHP-1) activity, leading to p-STAT3 and downstream cyclin B1 and Cdc2 downregulation. SC-43 augments SHP-1 activity by direct binding to N-SH2 and relief of its autoinhibition.
Cell Viability Assay
| Cell Line: | HuCCT-1, KKU-100, and CGCCA cells |
| Concentration: | 0 μM, 0.25 μM, 0.5 μM, 0.75 μM, 1 μM, 2.5 μM, 5 μM, 10 μM |
| Incubation Time: | 24 hours, 48 hours, 72 hours |
| Result: | Revealed the anti-proliferative effects in CCA cell lines in a dose-dependent manner after treating 24, 48 and 72 hours respectively. |
Cell Cycle Analysis
| Cell Line: | HuCCT-1, KKU-100, and CGCCA cells |
| Concentration: | 0 μM, 1 μM, 2.5 μM, 5 μM, 10 μM |
| Incubation Time: | 24 hours |
| Result: | Showed increased sub-G1 cells and G2-M arrest. |
Western Blot Analysis
| Cell Line: | HuCCT-1, KKU-100, and CGCCA cells |
| Concentration: | 0 μM, 1 μM, 2.5 μM, 5 μM, 10 μM |
| Incubation Time: | 24 hours |
| Result: | Demonstrated significant increase in cleaved caspase-3 and PARP level. |
SC-43 (10-30 mg/kg; oral gavage; daily; for 23 days; male NCr athymic nude mice) treatment exhibits xenograft tumor growth inhibition, p-STAT3 reduction and SHP-1 activity elevation.
| Animal Model: | Male NCr athymic nude mice (5-7 weeks of age) injected with HuCCT-1 cells |
| Dosage: | 10 mg/kg or 30 mg/kg |
| Administration: | Oral gavage; daily; for 23 days |
| Result: | Exhibited xenograft tumor growth inhibition, p-STAT3 reduction and SHP-1 activity elevation. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-136657 | SC-43 | 1 mg | 952元 | |
| 2024/01/25 | HY-136657 | SC-43 SC-43 | 1400989-25-4 | 5mg | 2500元 |