1400989-25-4

中文名称 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(3-(4-cyanophenoxy)phenyl)urea

英文名称 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 结构式

基本信息物理化学性质安全数据图谱信息常见问题列表

基本信息

中文别名

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

英文别名

SC-43
1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(3-(4-cyanophenoxy)phenyl)urea

所属类别

生物化工：激动剂抑制剂

物理化学性质

沸点462.0±45.0 °C(Predicted)

密度1.46±0.1 g/cm3(Predicted)

储存条件-20°C储存

溶解度DMSO: 250 mg/mL (578.97 mM)

酸度系数(pKa)12.92±0.70(Predicted)

形态固体

颜色White to off-white

安全数据

危险性符号(GHS)

GHS07

警示词警告

危险性描述H302-H319-H335-H315

防范说明P264-P280-P302+P352-P321-P332+P313-P362-P264-P280-P305+P351+P338-P337+P313P-P264-P270-P301+P312-P330-P501

图谱信息

SC-43(1400989-25-4)核磁图(¹HNMR)

常见问题列表

生物活性

SC-43 是索拉非尼sorafenib的衍生物，是一种 Src-homology protein tyrosine phosphatase-1 (SHP-1/PTPN6) 的激动剂，可减少肝纤维化。SC-43 可减少 p-STAT3 并诱导凋亡，具有抗肿瘤的活性。

靶点

Target	Value
SHP-1 ()
STAT3 ()

体外研究

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.

体内研究

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.