M3686 | TEAD1 inhibitor | Probechem Biochemicals

Chemical Structure : M3686

M3686 (M-3686)

Catalog No.: PC-23670Not For Human Use, Lab Use Only.

M3686 is a potent, selective TEAD1 inhibitor with IC50 of 51 nM in TEAD reporter assay, shows weaker binding to TEAD3, and negligible activity on TEAD2 and TEAD4.

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Biological Activity

M3686 is a potent, selective TEAD1 inhibitor with IC50 of 51 nM in TEAD reporter assay, shows weaker binding to TEAD3, and negligible activity on TEAD2 and TEAD4.
M3686 potently inhibits cell viability against YAP-dependent NCI-H226 cell line with IC50 of 0.06 uM.
M3686 (3, 10, and 30 mg/kg) shows strong anti-tumor effects in the NCI-H226 xenograft model.

Physicochemical Properties

M.Wt	429.40
Formula	C21H18F3N5O2
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
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Solubility	10 mM in DMSO
Chemical Name/SMILES	(R)-(3-hydroxypyrrolidin-1-yl)(2-methyl-4-(4-(trifluoromethyl)phenyl)-2,4-dihydro-[1,2,3]triazolo[4,5-b]indol-7-yl)methanone

References

1. Heinrich T, et al. J Med Chem. 2024 Dec 20. doi: 10.1021/acs.jmedchem.4c01949.

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M3686 (M-3686)

Biological Activity

Physicochemical Properties

References

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