VVD-133214 (VVD-214) | WRN inhibitor | Probechem Biochemicals

Chemical Structure : VVD-133214

CAS No.: 3026500-20-6

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

货号: 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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10 mg	￥4580	In stock
25 mg	￥7880	In stock
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生物&药学活性

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.

物理化学性质&存储条件

分子量	437.46
分子式	C20H21F2N3O4S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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.

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

生物&药学活性

物理化学性质&存储条件

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

生物&药学活性

物理化学性质&存储条件

参考文献

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