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TEAD-IN-21 is a potent, orally bioavailable pan-TEAD inhibitor with an IC50 of 3 nM. It effectively suppresses proliferation in Huh-7 cells and selectively downregulates TEAD-dependent downstream genes. In mouse models with liver cancer-derived tumor xenografts, TEAD-IN-21 leads to tumor regression. This compound is applicable for hepatocellular carcinoma (HCC) research.
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | TEAD-IN-21 is a potent, orally bioavailable pan-TEAD inhibitor with an IC50 of 3 nM. It effectively suppresses proliferation in Huh-7 cells and selectively downregulates TEAD-dependent downstream genes. In mouse models with liver cancer-derived tumor xenografts, TEAD-IN-21 leads to tumor regression. This compound is applicable for hepatocellular carcinoma (HCC) research. |
| Targets&IC50 | TEAD:3 nM |
| In vitro | TEAD-IN-21 (Compound C11) demonstrates moderate inhibitory effects on Bel-7402, SNU182, and Li-7 cells at concentrations of 0.1-100 μM, and exhibits optimal inhibition on Huh-7 cells. At concentrations of 0.3-40 μM over 14 days, it significantly reduces colony formation in these cells while showing minimal activity in TEAD-insensitive liver cancer cell lines. TEAD-IN-21 (0-40 μM) also downregulates TEAD downstream gene transcription levels in a dose-dependent manner. |
| In vivo | TEAD-IN-21 (Compound C11) administered orally at a dose of 50 mg/kg once daily for 20 consecutive days effectively inhibits the growth of Huh-7 xenograft tumors in a mouse model. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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