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Chemical Structure : VVD-133214
CAS No.: 3026500-20-6
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $298 | In stock | |
| 10 mg | $458 | In stock | |
| 25 mg | $788 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 437.46 | |
| Formula | C20H21F2N3O4S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
|
| Chemical Name/SMILES |
(S,E)-N-(1-cyclopropyl-3-(methylsulfonyl)allyl)-2-(1,1-difluoroethyl)-4-phenoxypyrimidine-5-carboxamide |
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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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