To evaluate the effects of TEAD inhibitors on the proliferation of NF2 wild-type cells. Results showed that 10 μM of VT103, VT107, and K-975 affected the proliferation of NF2 wild-type cell lines (mainly NCI-H28).
Pharmaceuticals (Basel). 2023 Nov 21;16(12):1635
NCI-H28
10 µM
4 days
To evaluate the effects of TEAD inhibitors on the proliferation of NF2 wild-type cells. Results showed that 10 μM of VT103, VT107, and K-975 affected the proliferation of NF2 wild-type cell lines (mainly NCI-H28).
Pharmaceuticals (Basel). 2023 Nov 21;16(12):1635
NCI-H2052
0.1-10 µM
4 days
To evaluate the inhibitory effects of TEAD inhibitors on the proliferation of NF2-deficient mesothelioma cells. Results showed that VT103, VT107, and K-975 exhibited the strongest inhibition of proliferation in the two NF2-deficient cell lines.
Pharmaceuticals (Basel). 2023 Nov 21;16(12):1635
NCI-H226
0.1-10 µM
4 days
To evaluate the inhibitory effects of TEAD inhibitors on the proliferation of NF2-deficient mesothelioma cells. Results showed that VT103, VT107, and K-975 exhibited the strongest inhibition of proliferation in the two NF2-deficient cell lines.
Pharmaceuticals (Basel). 2023 Nov 21;16(12):1635
HepG2
10 µM
4 hours
To evaluate the effects of TEAD inhibitors on the expression of YAP/TEAD target genes in Hippo pathway-proficient cells. Results showed that TEAD inhibition led to a partial reduction in AMOTL2, CTGF, and CYR61 mRNA expression.
Pharmaceuticals (Basel). 2023 Nov 21;16(12):1635
VT103 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Transverse aortic constriction (TAC) model
Intraperitoneal injection
20 mg/kg
Every other day for 28 days
To evaluate the effect of VT103 on TAC-induced cardiac remodeling. Results showed that VT103 treatment improved cardiac function, reduced cardiac hypertrophy and fibrosis, and decreased the expression of cardiac fibrotic markers α-SMA and galectin-3.
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