VT107

SKU: orb1694524

Description

VT-107 is a potent and selective inhibitor of TEAD autopalmitoylation, effectively disrupting the Hippo signaling pathway. This small molecule is a valuable research tool for studying oncogenic YAP/TAZ-TEAD activity in cancer biology, with applications in both in vitro cellular assays and in vivo xenograft models for therapeutic exploration.

Research Area

Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2417718-63-7
• MW: 435.44
• Purity: 99.92% (May vary between batches)
• Formula: C₂₅H₂₀F₃N₃O
• SMILES: C[C@H](NC(=O)c1ccc2c(cccc2c1)-c1ccc(cc1)C(F)(F)F)c1cccc(N)n1
• Target: YAP
• Solubility: DMSO:260 mg/mL (597.1 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (11.48 mM)

Bioactivity

• Target IC50:
  NCI-H226 cells:0.02 μM|pan-TEAD auto-palmitoylation:4.93 nM
• In Vivo:
  METHODS: VT107 was administered intravenously or orally at a dose of 10 mg/kg. Blood was drawn from the saphenous vein at designated time points. Compounds were quantified by LC/MS-MS using a QTRAP 6500 RESULTS The bioavailability of VT107 was 55%. The half-life after intravenous administration was 2.7 hours.
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• In Vitro:
  METHODS: HEK293T cells were treated with 3 μmol/L VT107 for 20 h. After incubation of cells with compounds and alkyne palmitate overnight, the relevant TEAD proteins were immunoprecipitated using specific TEAD antibodies, followed by click chemistry and streptavidin western blot analysis to examine the effects of these compounds on the palmitoylation of endogenous TEAD1, TEAD3, and TEAD4 proteins. RESULTS VT107 effectively blocked the palmitoylation of endogenous TEAD1 and TEAD3 proteins, and also effectively blocked the palmitoylation of endogenous TEAD4 protein. In addition, VT107 showed a strong inhibitory effect on the proliferation of NF2 mutant/deficient cell lines.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

YAP–TEAD, VT 107, VT107, VT-107

Compound Identifiers

PubChem CID

153583246