VT-103
| CAS No. | 2290608-13-6 | Cat. No. | BCP45566 |
| Name | VT-103 | ||
| Synonyms | VT 103; VT103; | ||
| Formula | C18H17F3N4O2S | M. Wt | 410.41 |
| Description | VT-103 is a potent and selective TEAD Auto-palmitoylation inhibitor that Inhibits Proliferation and Tumor Growth of NF2-deficient Mesothelioma. VT103 is a TEAD1-selective inhibitor. VT103 is an analog of VT101, which has 238 improved potency and good oral pharmacokinetics in mice. VT103 selectively inhibited endogenous TEAD1 palmitoylation in cells. VT103 significantly downregulated the expression of the Hippo pathway target genes, CTGF and CYR61, in the NF2-deficient NCI-H226 tumors in mice in a dose-dependent manner. VT103 showed excellent orally bioavailability and long half-lives, which inhibits tumor growth and also lead to shrinkage of established tumors in preclinical models of human mesothelioma CDX models deficient in functional Merlin. | ||
| Pathways | Wnt/Stem Cell | ||
Structure
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