TEAD-IN-21
TEAD-IN-21 is a potent and orally active pan-TEAD inhibitor with an IC50 of 3 nM. TEAD-IN-21 effectively inhibited the proliferation of Huh-7 cells. TEAD-IN-21 selectively downregulates TEAD-dependent downstream genes. TEAD-IN-21 achieves tumor regression in a liver cancer-derived tumor xenograft mice model. TEAD-IN-21 can be used in the research of hepatocellular carcinoma (HCC).
For research use only. We do not sell to patients.
- Formula: C16H15F3N6O2S
- Molecular Weight:412.39
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
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TEAD 3 nM (IC50) |
TEAD-IN-21 (Compound C11) (0.1-100 μM) has moderate inhibitory effects on Bel-7402, SNU182, and Li-7 cells, and its inhibitory effect is the best on Huh-7 cells[1].
TEAD-IN-21 (0.3-40 μM, 14 days) significantly reduces their colony formation, while exhibiting minimal activity against TEAD-insensitive HCC cell lines[1].
TEAD-IN-21 (0-40 μM) exerts a dose-dependent effect on downregulating the transcriptional levels of TEAD downstream genes CTGF and Cyr61[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Tmax | T1/2 | Cmax | AUC0-t | AUC0-∞ |
|---|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | p.o. | 6.0 h | 27.8 h | 448.3 ng/mL | 8191.4 ng·h/mL | 19621.0 ng·h/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Huh-7 xenograft tumor model established in nu/nu mice[1]
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Dosage:50 mg/kg
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Administration:Oral administration (p.o.), once daily for 20 days
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Result:Effectively inhibited the growth of HCC tumors in the body and had excellent safety profile.
Chemical Information
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Molecular Weight 412.39
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Formula C16H15F3N6O2S
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SMILES
CS(=O)(NC1=CC=C(NC2=CC=C(C(F)(F)F)C=C2)C(C3=NN(C)N=N3)=C1)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TEAD-IN-21 Related Classifications
HY-178098 Related Classifications
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