SMILES string
O=C(NC1=CC=C(C)C(OC2=CC=C(C=C2)Cl)=C1)C=C
assay
≥95% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Orally active, potent, irreversible pan-TEAD inhibitor that disrupts YAP1/TAZ-TEAD association and inhibits malignant pleural mesothelioma proliferation in vitro and in vivo.
K-975 is an orally active, potent, irreversible pan-TEAD inhibitor that disrupts YAP1/TAZ-TEAD interaction via covalent modification of TEAD palmitate-binding pocket (PBP) cysteine. K-975 suppresses NCI-H661 cellular TEAD transcriptional activity (IC50 ~100 nM by reporter assay) and selectively inhibits the proliferations of neurofibromin 2 (NF2)-deficient malignant pleural mesothelioma (MPM) cultures (IC50 ≤175 nM) over NF2-expressing MPM. K-975 suppressed tumor growth in MPM xenograft models in mice in vivo (35-300 mg/kg b.i.d. p.o. for 4 wks).
K-975 is an orally active, potent, irreversible pan-TEAD inhibitor that disrupts YAP1/TAZ-TEAD interaction via covalent modification of TEAD palmitate-binding pocket (PBP) cysteine. K-975 suppresses NCI-H661 cellular TEAD transcriptional activity (IC50 ~100 nM by reporter assay) and selectively inhibits the proliferations of neurofibromin 2 (NF2)-deficient malignant pleural mesothelioma (MPM) cultures (IC50 ≤175 nM) over NF2-expressing MPM. K-975 suppressed tumor growth in MPM xenograft models in mice in vivo (35-300 mg/kg b.i.d. p.o. for 4 wks).
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