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Merck
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重要文件

SML3445

Sigma-Aldrich

VT104

≥98% (HPLC)

同義詞:

(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

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About This Item

經驗公式(希爾表示法):
C25H19F3N2O
CAS號碼:
分子量::
420.43
分類程式碼代碼:
12352200
NACRES:
NA.21
暫時無法取得訂價和供貨情況

品質等級

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

2-8°C

SMILES 字串

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 密鑰

AAZUPSFRSHFTGV-INIZCTEOSA-N

生化/生理作用

Orally available pan-TEAD auto-palmitoylation inhibitor with anti-proliferation efficacy against mesothelioma with NF2 defect in cultures and in vivo.
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).

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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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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