VT-103 (CAT: I038128) is a potent and selective TEAD auto-palmitoylation inhibitor. It shows promising efficacy in inhibiting the proliferation and tumor growth of NF2-deficient mesothelioma. VT-103 is a TEAD1-selective inhibitor, downregulating Hippo pathway target genes. It exhibits good oral bioavailability, long half-lives, and inhibits tumor growth, leading to shrinkage of established tumors in preclinical models of human mesothelioma deficient in functional Merlin. VT-103 holds potential as a therapeutic agent and warrants further investigation as a treatment for NF2-deficient mesothelioma.
| Catalog Number | I038128 |
| CAS Number | 2290608-13-6 |
| Synonyms | VT-103; VT 103; VT103 |
| Molecular Formula | C18H17F3N4O2S |
| Purity | 98% |
| Solubility | To be determined |
| Appearance | Solid powder |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| IUPAC Name | N-methyl-3-(1-methyl-1H-imidazol-4-yl)-4-((4-(trifluoromethyl)phenyl)amino)benzenesulfonamide |
| InChI | InChI=1S/C18H17F3N4O2S/c1-22-28(26,27)14-7-8-16(15(9-14)17-10-25(2)11-23-17)24-13-5-3-12(4-6-13)18(19,20)21/h3-11,22,24H,1-2H3 |
| InChIKey | LLCVDQHLYHBAHR-UHFFFAOYSA-N |
| SMILES | CN1C=NC(C2=C(NC3=CC=C(C(F)(F)F)C=C3)C=CC(S(=O)(NC)=O)=C2)=C1 |
| Reference | Tang TT, Konradi AW, Feng Y, Peng X, Ma M, Li J, Yu FX, Guan KL, Post L. Small Molecule Inhibitors of TEAD Auto-palmitoylation Selectively Inhibit Proliferation and Tumor Growth of NF2-deficient Mesothelioma. Mol Cancer Ther. 2021 Apr 13:molcanther.0717.2020. doi: 10.1158/1535-7163.MCT-20-0717. Epub ahead of print. PMID: 33850002. |
