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BPI-460372

Chemical Structure : BPI-460372

CAS No.: 2762619-63-4

BPI-460372 (BPI460372)

Catalog No.: PC-23994Not For Human Use, Lab Use Only.

BPI-460372 is a potent, orally available, covalent, irreversible inhibitor of TEAD1/3/4, irreversibly binds to the cysteine residue in the TEAD palmitoylation pocket, preventing TEAD palmitoylation and inhibiting its biological function.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

BPI-460372 is a potent, orally available, covalent, irreversible inhibitor of TEAD1/3/4, irreversibly binds to the cysteine residue in the TEAD palmitoylation pocket, preventing TEAD palmitoylation and inhibiting its biological function.
BPI-460372 significantly inhibits the expression of a TEAD-responsive element reporter, as well as the mRNA of downstream target genes such as CTGF and CYR61 in NF2-deficient cells.
BPI-460372 strongly inhibited the proliferation of tumor cells harboring Hippo pathway aberrations.
BPI-460372 significantly suppressed tumor growth in NF2-deficient or LATS1/2 mutation xenograft models.

Physicochemical Properties

M.Wt 407.33
Formula C18H13F4N5O2
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
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-(1-(2-Fluoroacryloyl)azetidin-3-yl)-3-(4-(trifluoromethyl)phenyl)-1,3-dihydro-2H-imidazo[4,5-b]pyrazin-2-one

References

1. Xiaohong Han, et al. Cancer Res (2024) 84 (6_Supplement): 7575.

2. Hongling Shen, et al. Cancer Res (2023) 83 (7_Supplement): 501.

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