SML3686

MYF-03-176

≥98% (HPLC)

• Synonym(s): 2-Fluoro-1-[(3R,4R)-3-(2-pyrimidinylamino)-4-[[4-(trifluoromethyl)phenyl]methoxy]-1-pyrrolidinyl]-2-propen-1-one
• Empirical Formula (Hill Notation): C₁₉H₁₈F₄N₄O₂
• CAS Number: 2857937-59-6
• Molecular Weight: 410.37
• UNSPSC Code: 12352200
• NACRES: NA.21

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• storage condition: desiccated
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C

Description

Biochem/physiol Actions

MYF-03-176 is an orally active, potent, irreversible pan-TEAD inhibitor that disrupts YAP-TEAD association by targeting TEAD palmitate pocket for covalent binding. MYF-03-176 suppresses NCI-H226 cellular TEAD transcriptional activity (IC50 = 11 nM by TEAD reporter assay), blocking TEAD-mediated target genes expression (CTGF, CYR61, ANKRD1) and suppression (BMF). MYF-03-176 effectively inhibits Hippo signaling-driven human lung mesothelioma NCI-H226 proliferaton in cultures (IC50 = 9 nM in 5 days) and in a xenograft model in mice in vivo (35 or 75 mg/kg b.i.d. p.o. for 4 wks).

Orally active, potent, irreversible pan-TEAD inhibitor that disrupts YAP-TEAD association and inhibits Hippo signaling-driven cancer proliferation in vitro and in vivo.

Caution

Hygroscopic

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable