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Description: Potent pan-TEAD inhibitor
Chemical Name: N-[(1S)-1-(2-Pyridinyl)ethyl]-5-[4-(trifluoromethyl)phenyl]-2-naphthalenecarboxamide
Purity: ≥98% (HPLC)
Biological Activity for VT 104
VT 104 is a potent pan-TEAD (transcriptional enhanced associate domain) inhibitor (IC50 = 10.4 nM). VT 104 inhibits YAP/TAZ-TEAD promoted gene transcription by preventing the association between YAP/TAZ and TEAD. VT 104 blocks TEAD auto-palmitoylation. In vitro, VT 104 inhibits NF2-deficient mesothelioma cell proliferation, and growth of subcutaneous tumor xenografts in vivo. VT 104 is orally bioavailable.
Technical Data for VT 104
| M. Wt | 420.43 |
| Formula | C25H19F3N2O |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2417718-25-1 |
| PubChem ID | 146909371 |
| InChI Key | AAZUPSFRSHFTGV-INIZCTEOSA-N |
| Smiles | C(N[C@@H](C)C1=CC=CC=N1)(=O)C2=CC3=C(C(=CC=C3)C4=CC=C(C(F)(F)F)C=C4)C=C2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for VT 104
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 42.04 | 100 | |
| ethanol | 21.02 | 50 |
Preparing Stock Solutions for VT 104
The following data is based on the product molecular weight 420.43. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.38 mL | 11.89 mL | 23.79 mL |
| 5 mM | 0.48 mL | 2.38 mL | 4.76 mL |
| 10 mM | 0.24 mL | 1.19 mL | 2.38 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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Product Datasheets for VT 104
References for VT 104
References are publications that support the biological activity of the product.
Tang et al (2021) Small molecule inhibitors of TEAD auto-palmitoylation selectively inhibit proliferation and tumor growth of NF2-deficient mesothelioma. Mol.Cancer Ther. 20 986 PMID: 33850002
If you know of a relevant reference for VT 104, please let us know.
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Citations for VT 104
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Stem Cells Scientific Review
Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.
Stem Cells Poster
Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.
Pathways for VT 104
MAPK Signaling Pathway
The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.
Notch Signaling Pathway
The Notch pathway is involved in determination of cell fate, regulation of pattern formation and other developmental settings. Disrupted signaling can cause developmental defects and a range of adult pathologies.