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1400989-25-4

中文名稱 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(3-(4-cyanophenoxy)phenyl)urea
英文名稱 SC-43
CAS 1400989-25-4
分子式 C21H13ClF3N3O2
分子量 431.8
MOL 文件 1400989-25-4.mol
更新日期 2024/05/12 20:14:36
1400989-25-4 結(jié)構(gòu)式 1400989-25-4 結(jié)構(gòu)式

基本信息

中文別名
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
英文別名
SC-43
1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(3-(4-cyanophenoxy)phenyl)urea
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

沸點462.0±45.0 °C(Predicted)
密度1.46±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO: 250 mg/mL (578.97 mM)
酸度系數(shù)(pKa)12.92±0.70(Predicted)
形態(tài)固體
顏色White to off-white

圖譜信息

常見問題列表

生物活性
SC-43 是索拉非尼sorafenib的衍生物,是一種 Src-homology protein tyrosine phosphatase-1 (SHP-1/PTPN6) 的激動劑,可減少肝纖維化。SC-43 可減少 p-STAT3 并誘導(dǎo)凋亡,具有抗腫瘤的活性。
靶點
TargetValue
SHP-1
()
STAT3
()
體外研究

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.
體內(nèi)研究

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.
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