Orally available pan-TEAD auto-palmitoylation inhibitor with anti-proliferation efficacy against mesothelioma with NF2 defect in cultures and in vivo.
VT104 is an orally available pan-TEAD auto-palmitoylation inhibitor (3 μM; using TEAD isotype-overexpressing HEK293T) that blocks TEAD-mediated gene transcription (IC50 = 10.4 nM) by preventing its association with YAP/TAZ. VT104 selectively inhibits the proliferation of mesothelioma cultures with NF2 mutation (NCI-H2051 IC50 = 31.6 nM), deletion (NCI-H2373 IC50 = 25.6 nM) or deficiency (NCI-H226 IC50 = 16.1 nM), but not those with wild-type NF2. Oral administration is efficacious against human mesothelioma NCI-H226 tumor growth in mice in vivo (1-3 mg/kg/day).
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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Small Molecule Inhibitors of TEAD Auto-palmitoylation Selectively Inhibit Proliferation and Tumor Growth of NF2-deficient Mesothelioma
Tang TT, Konradi AW, Feng Y, Peng X, Ma M, Li J, Yu FX, Guan KL, Post L
Molecular Cancer Therapeutics, 20, 986-998 (2021)
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