SMO-IN-6
Anticancer agent 321 is a Smoothened (SMO) inhibitor with a human IC50 of 0.12 μM, enhanced aqueous solubility, good plasma and metabolic stability, moderate therapeutic index, preliminary safety profile, and moderate oral bioavailability in rats.Anticancer agent 321 binds to SMO’s 7-transmembrane helical channel, forming hydrogen bonds with Asp384 and hydrophobic/π-π interactions with His470, Phe391, Tyr394, stabilizing SMO’s inactive conformation to inhibit Hedgehog/GLI signaling.Anticancer agent 321 inhibits proliferation, suppresses colony formation, induces apoptosis, and downregulates Hedgehog/GLI pathway target genes GLI1, GLI2, Ptch1, HHip in cancer cells.Anticancer agent 321 inhibits tumor growth, downregulates Ki67 and SOX2, and upregulates cleaved-caspase 3 in tumor tissues.Anticancer agent 321 can be used for the research of cutaneous squamous cell carcinoma.
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- Formule: C23H26Cl2N2O3
- Masse moléculaire:449.37
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
SMO-IN-6 (Compound 16) (72 h) potently inhibits the proliferation of A431 cutaneous squamous cell carcinoma cells, with a GI50 of 1.4 μM and a therapeutic index of 31 relative to non-tumorigenic HaCaT skin cells[1].
SMO-IN-6 (1-4 μM; 14 days) inhibits long-term colony formation of A431 cutaneous squamous cell carcinoma cells in a dose-dependent manner, with an inhibition rate exceeding 95% at 4 μM[1].
SMO-IN-6 (1 μM) potently downregulates the expression of Hedgehog/GLI pathway target genes Gli1, Gli2, Ptch1 and HHip in A431 cutaneous squamous cell carcinoma cells[1].
SMO-IN-6 (1-4 μM; 16 h) induces apoptosis in A431 cutaneous squamous cell carcinoma cells in a dose-dependent manner, with the apoptosis rate reaching 93% at the concentration of 4 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A431 cutaneous squamous cell carcinoma cells
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Concentration:1, 2 and 4 μM
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Incubation Time:14 day
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Result:Inhibited A431 colony formation in a dose-dependent manner: 1 μM reduced colony formation by over 50%, and 4 μM inhibited over 95% of colony formation.
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Cell Line:A431 cutaneous squamous cell carcinoma cells
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Concentration:1, 2 and 4 μM
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Incubation Time:16 h
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Result:Induced apoptosis in A431 cells in a dose-dependent manner: 1 μM induced apoptosis in 38% of cells, 2 μM in 54% of cells, and 4 μM in up to 93% of cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (female, 6-8 weeks old, 18-20 g, subcutaneously injected with A431 cells)[1]
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Dosage:10 mg/kg; 25 mg/kg
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Administration:i.p.; 2on1off dosing regimen; 14 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 30%.
Achieved a TGI rate of 56%.
Induced ~40% TUNEL-positive apoptotic cells.
Significantly downregulated GLI1, Ki67, and SOX2 levels in tumor tissues.
Significantly upregulated cleaved-caspase 3 levels in tumor tissues.
Caused no significant body weight loss, morphological abnormalities in major organs, or hematological toxicity.
Chemical Information
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Masse moléculaire 449.37
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Formule C23H26Cl2N2O3
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SMILES
C[C@]1(O[C@H](COC2=CC=C(N3CC4CCC(N4)C3)C=C2)CO1)C5=CC=C(Cl)C=C5Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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