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VVD-133214

Chemical Structure : VVD-133214

CAS No.: 3026500-20-6

VVD-133214 (VVD-214, VVD133214, RO7589831, VVD214)

Catalog No.: PC-22121Not For Human Use, Lab Use Only.

VVD-133214 (VVD214, RO7589831) is a potent, selective, covalent allosteric inhibitor of WRN helicase, covalently engages cysteine 727 of WRN in a nucleotide cooperative manner and inhibits ATP hydrolysis and helicase activity.

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Biological Activity

VVD-133214 (VVD214, RO7589831) is a potent, selective, covalent allosteric inhibitor of WRN helicase, covalently engages cysteine 727 of WRN in a nucleotide cooperative manner and inhibits ATP hydrolysis and helicase activity.
VVD-214 treatment causes widespread double-stranded DNA breaks, nuclear swelling, and cell death in MSI-high, but not microsatellite stable cells.
VVD-214 exhibits robust tumor regression in multiple MSI-high colorectal cancer cell lines and patient derived xenograft models, including models derived from patients progressing on immune checkpoint therapies.

Physicochemical Properties

M.Wt 437.46
Formula C20H21F2N3O4S
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

(S,E)-N-(1-cyclopropyl-3-(methylsulfonyl)allyl)-2-(1,1-difluoroethyl)-4-phenoxypyrimidine-5-carboxamide

References

1. Shota Kikuchi, et al. Cancer Res (2024) 84 (7_Supplement): ND11.
2. Baltgalvis KA, et al. Nature. 2024 Apr 24. doi: 10.1038/s41586-024-07318-y.

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