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Safety Information

SML3686

Sigma-Aldrich

MYF-03-176

≥98% (HPLC)

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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:
Molecular Weight:
410.37
UNSPSC Code:
12352200
NACRES:
NA.21

Quality Level

Assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

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).

Caution

Hygroscopic

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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Covalent disruptor of YAP-TEAD association suppresses defective Hippo signaling
eLife, 11, e78810-e78810 (2022)

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