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| Product Name: | SC-43 | | Synonyms: | 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(3-(4-cyanophenoxy)phenyl)urea;SC-43;Urea, N-[4-chloro-3-(trifluoromethyl)phenyl]-N'-[3-(4-cyanophenoxy)phenyl]-;antiproliferative,Inhibitor,SC-43,SHP-1,PTPN6,Phosphatase,Apoptosis,caspase-3,SC 43,anti-fibrotic,p-STAT3,anticancer,orally,SC43,PARP,STAT,inhibit | | CAS: | 1400989-25-4 | | MF: | C21H13ClF3N3O2 | | MW: | 431.8 | | EINECS: | | | Product Categories: | | | Mol File: | 1400989-25-4.mol |  |
| | SC-43 Chemical Properties |
| 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 |
| | SC-43 Usage And Synthesis |
| 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
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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
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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. | | | target | | Target | Value | SHP-1
() | STAT3
() |
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| | SC-43 Preparation Products And Raw materials |
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