SC-43

生物活性靶点体外研究体内研究 SC-43 试剂级价格

SC-43

CAS号:1400989-25-4
英文名:SC-43
中文名:SC-43
CBNumber:CB94801426
分子式:C21H13ClF3N3O2
分子量:431.8
MOL File:1400989-25-4.mol

SC-43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 :Store at -20°C
溶解度 :DMSO: 250 mg/mL (578.97 mM)
形态 :A solid
酸度系数(pKa) :12.92±0.70(Predicted)
颜色 :White to off-white

SC-43性质、用途与生产工艺

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.