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质量水平
方案
≥98% (HPLC)
表单
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
InChI
1S/C25H19F3N2O/c1-16(23-7-2-3-14-29-23)30-24(31)19-10-13-22-18(15-19)5-4-6-21(22)17-8-11-20(12-9-17)25(26,27)28/h2-16H,1H3,(H,30,31)/t16-/m0/s1
InChI key
AAZUPSFRSHFTGV-INIZCTEOSA-N
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).
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
从最新的版本中选择一种：
分析证书(COA)
Lot/Batch Number
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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