| Identification | Back Directory | [Name]
VVD-133214 | [CAS]
3026500-20-6 | [Synonyms]
RO7589831
VVD-133214
VVD-214 (Synonyms: RO7589831
(S,E)-N-(1-cyclopropyl-3-(methylsulfonyl)allyl)-2-(1,1-difluoroethyl)-4-phenoxypyrimidine-5-carboxamide | [Molecular Formula]
C20H21F2N3O4S | [MOL File]
3026500-20-6.mol | [Molecular Weight]
437.46 |
| Chemical Properties | Back Directory | [Boiling point ]
627.5±55.0 °C(predicted) | [density ]
1.355±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | [form ]
Solid | [pka]
10.95±0.46(predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
VVD-214 is a synthetic lethal allosteric inhibitor of WRN helicase with an IC50 of 0.1316 μM. VVD-214 covalently binds to cysteine 727 of WRN and inhibits ATP hydrolysis and helicase activity. VVD-214 is potent in causing double-stranded DNA breaks, nuclear swelling, and cell death in high microsatellite instability (MSI) cancers[1][2]. | [References]
[1] Kikuchi S, et al. Abstract ND11: Chemoproteomic-enabled discovery of VVD-214, a synthetic lethal allosteric inhibitor of WRN helicase[J]. Cancer Research, 2024, 84(7_Supplement): ND11-ND11.
[2] Kikuchi S, et al., Pharmaceutical compositions comprising wrn helicase inhibitors. WO2024010782. |
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