VT103 是 VT101 的类似物，是一种具有口服活性和选择性的TEAD1蛋白棕榈酰化抑制剂。 VT103 抑制YAP/TAZ-TEAD促进的基因转录，阻断TEADauto-palmitoylation，阻断YAP/TAZ和TEAD之间的相互作用。VT103 可用于癌症研究。

VT103, an analog of VT101, is an orally active and selective TEAD1 protein palmitoylation inhibitor. VT103 inhibits YAP/TAZ-TEAD promoted gene transcription, blocks TEAD auto-palmitoylation, and disrupts interaction between YAP/TAZ and TEAD. VT103 can be used for the research of cancer [1].

VT103 (HEK293T cells; 3 μM) appeares to be TEAD1-selective, as it does not block palmitoylation of TEAD2, TEAD3, or TEAD4. VT103 (NF2-deficient NCI-H226 cells; 3 mmol/L; 4 or 24 hours) selectively disrupts YAP–TEAD1 interaction [1]. VT103 results in the disappearance of palmitoylated TEAD1 with a concomitant increase in unpalmitoylated TEAD1 [1]. VT103 shows an IC 50 of 1.02 nM in YAP reporter assay [1].

VT103 (0.3~10 mg/kg; p.o. once per day) blocks tumor growth even at 0.3 mg/kg [1]. Pharmacokinetics of VT103 in mice [1] Dose IV PO 7 mg/kg T1/2 (hours) Vdss (L/kg) CI(mL/min/kg) AUC 0-24 hours (μg*h/mL) AUC 0-24 hours (μg*h/mL) Oral availability (%) C max (ng/mL) C 24 hours (ng/mL) 13.2 4.5 4.7 20.0 14.9 75 896 (1 hour) 340 Animal Model: NCI-H226-tumor bearing mice [1] Dosage: 0.3~10 mg/kg Administration: P.o. once per day Result: Blocked tumor growth even at 0.3 mg/kg.

2290608-13-6

C18H17F3N4O2S

410.41

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years