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Merck
CN

SML3445

Sigma-Aldrich

VT104

≥98% (HPLC)

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别名:
(S)-N-(l-(Pyridin-2-yl)ethyl)-5-(4-(trifluoromethyl)phenyl)-2-naphthamide, N-[(1S)-1-(2-Pyridinyl)ethyl]-5-[4-(trifluoromethyl)phenyl]-2-naphthalenecarboxamide, VT-104
经验公式(希尔记法):
C25H19F3N2O
分子量:
420.43
UNSPSC代码:
12352200
NACRES:
NA.21

质量水平

检测方案

≥98% (HPLC)

形式

powder

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

2-8°C

SMILES字符串

FC(F)(C1=CC=C(C2=CC=CC3=CC(C(N[C@H](C4=NC=CC=C4)C)=O)=CC=C23)C=C1)F

生化/生理作用

VT104 is an orally available pan-TEAD auto-palmitoylation inhibitor (3 μM; using TEAD isotype-overexpressing HEK293T) that blocks TEAD-mediated gene transcription (IC50 = 10.4 nM) by preventing its association with YAP/TAZ. VT104 selectively inhibits the proliferation of mesothelioma cultures with NF2 mutation (NCI-H2051 IC50 = 31.6 nM), deletion (NCI-H2373 IC50 = 25.6 nM) or deficiency (NCI-H226 IC50 = 16.1 nM), but not those with wild-type NF2. Oral administration is efficacious against human mesothelioma NCI-H226 tumor growth in mice in vivo (1-3 mg/kg/day).

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

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Small Molecule Inhibitors of TEAD Auto-palmitoylation Selectively Inhibit Proliferation and Tumor Growth of NF2-deficient Mesothelioma
Tang TT, Konradi AW, Feng Y, Peng X, Ma M, Li J, Yu FX, Guan KL, Post L
Molecular Cancer Therapeutics, 20, 986-998 (2021)

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