SML3445

VT104

≥98% (HPLC)

• Synonym(e): (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
• Empirische Formel (Hill-System): C₂₅H₁₉F₃N₂O
• CAS-Nummer: 2417718-25-1
• Molekulargewicht: 420.43
• UNSPSC-Code: 12352200
• NACRES: NA.21

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 2 mg/mL, clear
• Lagertemp.: 2-8°C
• SMILES String: 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
• InChIKey: AAZUPSFRSHFTGV-INIZCTEOSA-N

Beschreibung

Biochem./physiol. Wirkung

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).

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable