1400989-25-4
1400989-25-4 結(jié)構(gòu)式
基本信息
1-(4-氯-3-(三氟甲基)苯基)-3-(3-(4-氰基苯氧基)苯基)脲
1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(3-(4-cyanophenoxy)phenyl)urea
物理化學性質(zhì)
常見問題列表
| 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. |