Identification | Back Directory | [Name]
1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(3-(4-cyanophenoxy)phenyl)urea | [CAS]
1400989-25-4 | [Synonyms]
SC-43 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(3-(4-cyanophenoxy)phenyl)urea | [Molecular Formula]
C21H13ClF3N3O2 | [MDL Number]
MFCD31380911 | [MOL File]
1400989-25-4.mol | [Molecular Weight]
431.8 |
Chemical Properties | Back Directory | [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 |
Hazard Information | Back Directory | [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:
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HuCCT-1, KKU-100, and CGCCA cells
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Concentration:
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0 μM, 1 μM, 2.5 μM, 5 μM, 10 μM
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Incubation Time:
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24 hours
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Result:
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Showed increased sub-G1 cells and G2-M arrest.
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Western Blot Analysis
Cell Line:
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HuCCT-1, KKU-100, and CGCCA cells
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Concentration:
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0 μM, 1 μM, 2.5 μM, 5 μM, 10 μM
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Incubation Time:
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24 hours
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Result:
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Demonstrated significant increase in cleaved caspase-3 and PARP level.
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| [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. | div> | [target]
Target | Value | SHP-1 () | STAT3 () |
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Company Name: |
DC Chemicals
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Tel: |
021-58447131 13564518121 |
Website: |
http://m.is0513.com/ShowSupplierProductsList927327/0.htm |
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