SC-43

CAS NO.：1400989-25-4
Empirical Formula: C21H13ClF3N3O2
Molecular Weight: 431.8
MDL number: MFCD31380911
Update Date: 2024-11-19 20:33:22

What is SC-43?

Biological Activity

SC-43 is a derivative of sorafenib, an agonist of Src-homology protein tyrosine phosphatase-1 (SHP-1/PTPN6), which reduces liver fibrosis. SC-43 can reduce p-STAT3 and induce apoptosis, and has antitumor activity.

in vitro

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.
Its treatment shows increased sub-G1 cells and G2-M arrest, indicating SC-43 induced differential apoptotic effects in these cell lines.
Its (0-10 μM; 24 hours; HuCCT-1, KKU-100, and CGCCA cells) treatment demonstrates significant increase in cleaved caspase-3 and PARP level.
Its activates SH2 domain-containing phosphatase 1 (SHP-1) activity, leading to p-STAT3 and downstream cyclin B1 and Cdc2 downregulation. Its augments SHP-1 activity by direct binding to N-SH2 and relief of its autoinhibition.

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.

in vivo

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.

Properties of SC-43

Boiling point:	462.0±45.0 °C(Predicted)
Density	1.46±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO: 250 mg/mL (578.97 mM)
form	A solid
pka	12.92±0.70(Predicted)
color	White to off-white