VT103

SKU: orb1687961

Description

VT103 is an orally bioavailable TEAD auto-palmitoylation inhibitor that disrupts the YAP/TAZ-TEAD transcriptional complex. This small molecule shows potential antitumor activity and is utilized in research models of cancers such as HER2-positive breast cancer, triple-negative breast cancer, and prostate cancer.

Research Area

Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2290608-13-6
• MW: 410.41
• Purity: 99.58% (May vary between batches)
• Formula: C₁₈H₁₇F₃N₄O₂S
• SMILES: CNS(=O)(=O)c1ccc(Nc2ccc(cc2)C(F)(F)F)c(c1)-c1cn(C)cn1
• Target: YAP
• Solubility: DMSO:50 mg/mL (121.83 mM);10% DMSO+90% Corn Oil:2.5 mg/mL (6.09 mM)

Bioactivity

• In Vivo:
  VT103 (0.3~10 mg/kg; p.o.; once daily; NCI-H226-tumor-bearing mice) inhibits tumor growth, with efficacy observed at 0.3 mg/kg. Pharmacokinetics of VT103 in mice.
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• In Vitro:
  VT103 (3 mmol/L; 4 or 24 h; NF2-deficient NCI-H226 cells) selectively disrupts YAP–TEAD1 interaction. VT103 (3 μM; HEK293T cells) appeared to be TEAD1-selective, as it does not block palmitoylation of TEAD2, TEAD3, or TEAD4. VT103 results in the disappearance of palmitoylated TEAD1 with a concomitant increase in unpalmitoylated TEAD1. VT103 shows an IC50 of 1.02 nM in the YAP reporter assay.
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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 103, VT103, VT-103

Compound Identifiers

PubChem CID

137534047