VT103 (VT-103)

Chemical Structure : VT103

CAS No.: 2290608-13-6

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货号: PC-72506Not For Human Use, Lab Use Only.

VT103 (VT-103) is a specific small molecule inhibitor of YAP/TAZ-TEAD-dependent transcription with IC50 of 1.2 nM in YAP reporter assay, selectively blocks TEAD1 auto-palmitoylation.

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生物&药学活性

VT103 (VT-103) is a specific small molecule inhibitor of YAP/TAZ-TEAD-dependent transcription with IC50 of 1.2 nM in YAP reporter assay, selectively blocks TEAD1 auto-palmitoylation.
VT103 appears to be TEAD1-selective, as it does not block palmitoylation of TEAD2, TEAD3, or TEAD4 in HEK293T cells transfected with plasmid expressing MYC-tagged full-length TEAD1, TEAD2, TEAD3, or TEAD4 protein, with no effect on RAS palmitoylation.
VT103 selectively binds directly to TEAD1 in the central lipid pocket, reduces YAP interaction with TEAD1 but not TEAD4 in NF2-mutant NCI-H2373 cells.
VT103 blocked the proliferation of NF2-deficient or NF2-mutated mesothelioma cell lines, 100- to 1,000-fold less activity in NF2 wild-type mesothelioma cells.
VT103 (3 mg/kg once daily, oral) block growth of NF2-deficient mesothelioma xenografts, exhibited strong antitumor efficacy, leading to tumor regression, even at 1 and 0.3 mg/kg once daily.

物理化学性质&存储条件

分子量	410.415
分子式	C18H17F3N4O2S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-methyl-3-(1-methyl-1H-imidazol-4-yl)-4-((4-(trifluoromethyl)phenyl)amino)benzenesulfonamide

参考文献

1. Tracy T Tang, et al. Mol Cancer Ther. 2021 Jun;20(6):986-998.

VT103 (VT-103)

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VT103 (VT-103)

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